Chal Micro

54
European Journal of Medicinal Chemistry 44 (2009) 5131–5184 B (E)–N' –[(E)–2–Butenoyl]–2–butenoylhy- drazide – Anti–genotoxic hydrazide from Crinum defixum, 2754 (Phenylsulfonyl)phenyl moiety – Synthesis, characterization and antibacterial activity of some triazole Mannich bases carrying diphenylsulfone moieties, 3083 – Synthesis, characterization and evaluation of antibac- terial activity of some thiazolo[3,2–b] [1,2,4]triazole incorporating diphenylsul- fone moieties, 4752 (S)–1,10–Bi–2–naphthol [(S)–BINOL] Synthesis of novel carbazole based macro- cyclic amides as potential antimicrobial agents, 3040 1,10–Phenanthroline – Antitumour activity of novel 1,10–phenanthroline and 5–amino–1,10–phenanthroline derivatives, 2720 Cytotoxicity and effects of 1,10–phenanthroline and 5–amino–1,10– phenanthroline derivatives on some immunocompetent cells, 5099 1,2,3,4–Tetrahydroisoquinoline – Facile syn- thesis and in vitro properties of 1–alkyl– and 1–alkyl– N–propargyl–1,2,3,4–tetrahy- droisoquinoline derivatives on PC12 cells, 4034 1,2,3–Triazole derivatives – Antiviral evaluation of N–amino–1,2,3–triazoles against Cantagalo virus replication in cell culture, 3777 1,2,3–Triazole – Synthesis, HIV–RT inhibitory activity and SAR of 1–benzyl–1H1,2,3–triazole derivatives of carbohydrates, 373 1,2,3–Triazoles – Synthesis and cytotoxic profile of glycosyl–triazole linked to 1,2,4–oxadiazole moiety at C–5 through a straight–chain carbon and oxygen atoms, 3571 1,2,4–Oxadiazoles – Synthesis, analgesic and anti–inflammatory activities of novel 3–(4–acetamido–benzyl)–5–substitut- ed–1,2,4–oxadiazoles, 794 – Synthesis and cytotoxic profile of glycosyl–triazole linked to 1,2,4–oxadiazole moiety at C–5 through a straight–chain carbon and oxygen atoms, 3571 1,2,4–Thiadiazole – Synthesis and anticon- vulsant activity of some substituted 1,2,4–thiadiazoles, 1100 1,2,4–Triazine – Synthesis of some novel pyrazolo[3,4–b]pyridine and pyrazolo [3,4–d]pyrimidine derivatives bearing 5,6–diphenyl–1,2,4–triazine moiety as potential antimicrobial agents, 4385 1,2,4–Triazino[4,3–a]quinolin–1–one Design, synthesis of 8–alkoxy–5,6–dihy- dro–[1,2,4]triazino[4,3–a]quinolin–1–ones with anticonvulsant activity, 1265 1,2,4–Triazinone – Synthesis and antibacteri- al activity of some new thiadiaza/triaza- phospholes, thiadiaza/triaza/tetrazaphos- phinines and thiadiaza/tetrazaphosphepines containing 1,2,4–triazinone moiety, 4539 1,2,4–Triazole – Design, synthesis and molecu- lar modeling study of acylated 1,2,4–tria- zole–3–acetates with potential anti–inflamma- tory activity, 117 – Synthesis of some new 1,2,4–triazoles, their Mannich and Schiff bases and evaluation of their antimicrobial activities, 1057 – Synthesis of some new 1,3,4–thiadiazol–2–ylmethyl–1,2,4– triazole derivatives and investigation of their antimicrobial activities, 2896 – Synthesis, structure elucidation and antitumour activity of N–substituted amides of 3–(3–ethyl- thio–1,2,4–triazol–5–yl)propenoic acid, 3788 – Synthesis of some new 1,2,4–triazoles start- ing from isonicotinic acid hydrazide and eval- uation of their antimicrobial activities, 4362 – Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4–triazole moiety, 4637 – Synthesis and antibacterial activity of some novel bis–1,2,4–triazolo [3,4–b]–1,3,4–thiadiazoles and bis–4–thiazo- lidinone derivatives from terephthalic dihy- drazide, 5112 1,2,4–Triazoles – Synthesis, cytotoxicity and effects of some 1,2,4–triazole and 1,3,4–thiadiazole derivatives on immuno- competent cells, 63 – Synthesis, antimicro- bial and cytotoxic activities of 1,3,4–oxadi- azoles, 1,3,4–thiadiazoles and 1,2,4–tria- zoles, 2106 – Regioselective reaction: Synthesis, characterization and pharmaco- logical studies of some new Mannich bases derived from 1,2,4–triazoles, 3784 – Synthesis and antitumor activity studies of some new fused 1,2,4–triazole derivatives carrying 2,4–dichloro–5–fluorophenyl moi- ety, 5066 1,2,4–Triazol–3–thiones – Synthesis of sub- stituted–phenyl–1,2,4–triazol–3–thione analogues with modified d–glucopyranosyl residues and their antiproliferative activi- ties, 4716 1,2,4–Triazolo – Synthesis of some new 4–styryltetrazolo[1,5–a]quinoxaline and 1–substituted–4–styryl[1,2,4]triazolo[4,3–a ]quinoxaline derivatives as potent anticon- vulsants, 1135 1,2,4–Triazolo[4,3–a]quinoline – Design and synthesis of 5–alkoxy–[1,2,4]triazolo [4,3–a]quinoline derivatives with anticon- vulsant activity, 954 1,2,8,9–Tetraazadispiro[4.1.4.2]tride- ca–2,9–dien–6–ones – Regioselective synthetic approaches towards 1,2,8,9– tetraazadispiro[4.1.4.2]trideca–2,9–dien– 6–ones of potential antimicrobial proper- ties, 2447 1,2–Benzothiazine–3–carbohydrazide 1,1–dioxides – A facile synthesis of novel biologically active 4–hydroxy–N'–(benzyli- dene)–2H–benzo[e][1,2]thiazine–3–carbo- hydrazide 1,1–dioxides, 1311 1,2–Oxazines – Synthesis of new series of 5,6–dihydro–4H–1,2–oxazines via hetero Diels–Alder reaction and evaluation of antimicrobial activity, 280 1,3,4–Oxadiazin–5(6H)–ones Novel 4H–1,3,4–oxadiazin–5(6H)–ones with hydrophobic and long alkyl chains: Design, synthesis, and bioactive diversity on inhibi- tion of monoamine oxidase, chitin biosyn- thesis and tumor cell, 2113 1,3,4–Oxadiazole – Synthesis of some new 1,2,4–triazoles, their Mannich and Schiff bases and evaluation of their antimicrobial activities, 1057 – A new type of five–mem- bered heterocyclic inhibitors of basic metal- locarboxypeptidases, 3266 – Fenbufen based 3–[5–(substituted aryl)–1,3,4–oxadia- zol–2–yl]–1–(biphenyl–4–yl)propan–1–one s as safer antiinflammatory and analgesic agents, 3798 – Synthesis and pharmacolog- ical evaluation of 1,3,4–oxadiazole bearing bis(heterocycle) derivatives as anti–inflam- matory and analgesic agents, 3898 – Synthesis, physicochemical properties and antimicrobial activity of some new benzim- idazole derivatives, 4028 – Synthesis of some new 1,2,4–triazoles starting from isonicotinic acid hydrazide and evaluation of their antimicrobial activities, 4362 1,3,4–Oxadiazole/thiadiazoles – Synthesis and antibacterial activity of some novel bis–1,2,4–triazolo[3,4–b]–1,3,4–thiadia- zoles and bis–4–thiazolidinone derivatives from terephthalic dihydrazide, 5112 1,3,4–Oxadiazoles – Synthesis, antimicrobial and cytotoxic activities of 1,3,4–oxadia- zoles, 1,3,4–thiadiazoles and 1,2,4–tria- zoles, 2106 – Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadia- zoles/thiadiazoles/triazoles, 2313 Aroylpropionic acid based 2,5–disubstitut- ed–1,3,4–oxadiazoles: Synthesis and their anti–inflammatory and analgesic activities, 2372 1,3,4–thiadiazines – Synthesis and antitumor activity studies of some new fused 1,2,4–tri- azole derivatives carrying 2,4–dichloro– 5–fluorophenyl moiety, 5066 1,3,4–Thiadiazole – Synthesis of some new 1,2,4–triazoles, their Mannich and Schiff bases and evaluation of their antimicrobial Keyword index doi:10.1016/S0223-5234(09)00568-6 Available online at www.sciencedirect.com http://www.elsevier.com/locate/ejmech

Transcript of Chal Micro

Page 1: Chal Micro

European Journal of Medicinal Chemistry 44 (2009) 5131–5184

B(E)–N'–[(E)–2–Butenoyl]–2–butenoylhy-

drazide – Anti–genotoxic hydrazide fromCrinum defixum, 2754

(Phenylsulfonyl)phenyl moiety – Synthesis,characterization and antibacterial activity ofsome triazole Mannich bases carryingdiphenylsulfone moieties, 3083 – Synthesis,characterization and evaluation of antibac-terial activity of some thiazolo[3,2–b][1,2,4]triazole incorporating diphenylsul-fone moieties, 4752

(S)–1,10–Bi–2–naphthol [(S)–BINOL] –Synthesis of novel carbazole based macro-cyclic amides as potential antimicrobialagents, 3040

1,10–Phenanthroline – Antitumour activityof novel 1,10–phenanthroline and5–amino–1,10–phenanthroline derivatives,2720 – Cytotoxicity and effects of1,10–phenanthroline and 5–amino–1,10–phenanthroline derivatives on someimmunocompetent cells, 5099

1,2,3,4–Tetrahydroisoquinoline – Facile syn-thesis and in vitro properties of 1–alkyl– and1–alkyl–N–propargyl–1,2,3,4–tetrahy-droisoquinoline derivatives on PC12 cells,4034

1,2,3–Triazole derivatives – Antiviral evaluationof N–amino–1,2,3–triazoles against Cantagalovirus replication in cell culture, 3777

1,2,3–Triazole – Synthesis, HIV–RT inhibitoryactivity and SAR of 1–benzyl–1H–1,2,3–triazole derivatives of carbohydrates, 373

1,2,3–Triazoles – Synthesis and cytotoxicprofile of glycosyl–triazole linked to1,2,4–oxadiazole moiety at C–5 through astraight–chain carbon and oxygen atoms,3571

1,2,4–Oxadiazoles – Synthesis, analgesic andanti–inflammatory activities of novel3–(4–acetamido–benzyl)–5–substitut-ed–1,2,4–oxadiazoles, 794 – Synthesis andcytotoxic profile of glycosyl–triazole linkedto 1,2,4–oxadiazole moiety at C–5 through astraight–chain carbon and oxygen atoms,3571

1,2,4–Thiadiazole – Synthesis and anticon-vulsant activity of some substituted1,2,4–thiadiazoles, 1100

1,2,4–Triazine – Synthesis of some novelpyrazolo[3,4–b]pyridine and pyrazolo[3,4–d]pyrimidine derivatives bearing5,6–diphenyl–1,2,4–triazine moiety aspotential antimicrobial agents, 4385

1,2,4–Triazino[4,3–a]quinolin–1–one –Design, synthesis of 8–alkoxy–5,6–dihy-dro–[1,2,4]triazino[4,3–a]quinolin–1–oneswith anticonvulsant activity, 1265

1,2,4–Triazinone – Synthesis and antibacteri-al activity of some new thiadiaza/triaza-phospholes, thiadiaza/triaza/tetrazaphos-phinines and thiadiaza/tetrazaphosphepinescontaining 1,2,4–triazinone moiety, 4539

1,2,4–Triazole – Design, synthesis and molecu-lar modeling study of acylated 1,2,4–tria-zole–3–acetates with potential anti–inflamma-tory activity, 117 – Synthesis of some new1,2,4–triazoles, their Mannich and Schiffbases and evaluation of their antimicrobialactivities, 1057 – Synthesis of some new1,3,4–thiadiazol–2–ylmethyl–1,2,4–triazole derivatives and investigation of theirantimicrobial activities, 2896 – Synthesis,structure elucidation and antitumour activityof N–substituted amides of 3–(3–ethyl-thio–1,2,4–triazol–5–yl)propenoic acid, 3788– Synthesis of some new 1,2,4–triazoles start-ing from isonicotinic acid hydrazide and eval-uation of their antimicrobial activities, 4362 –Synthesis and antimicrobial activities of novelquinoline derivatives carrying 1,2,4–triazolemoiety, 4637 – Synthesis and antibacterialactivity of some novel bis–1,2,4–triazolo[3,4–b]–1,3,4–thiadiazoles and bis–4–thiazo-lidinone derivatives from terephthalic dihy-drazide, 5112

1,2,4–Triazoles – Synthesis, cytotoxicity andeffects of some 1,2,4–triazole and1,3,4–thiadiazole derivatives on immuno-competent cells, 63 – Synthesis, antimicro-bial and cytotoxic activities of 1,3,4–oxadi-azoles, 1,3,4–thiadiazoles and 1,2,4–tria-zoles, 2106 – Regioselective reaction:Synthesis, characterization and pharmaco-logical studies of some new Mannich basesderived from 1,2,4–triazoles, 3784 –Synthesis and antitumor activity studies ofsome new fused 1,2,4–triazole derivativescarrying 2,4–dichloro–5–fluorophenyl moi-ety, 5066

1,2,4–Triazol–3–thiones – Synthesis of sub-stituted–phenyl–1,2,4–triazol–3–thioneanalogues with modified d–glucopyranosylresidues and their antiproliferative activi-ties, 4716

1,2,4–Triazolo – Synthesis of some new4–styryltetrazolo[1,5–a]quinoxaline and1–substituted–4–styryl[1,2,4]triazolo[4,3–a]quinoxaline derivatives as potent anticon-vulsants, 1135

1,2,4–Triazolo[4,3–a]quinoline – Design andsynthesis of 5–alkoxy–[1,2,4]triazolo[4,3–a]quinoline derivatives with anticon-vulsant activity, 954

1,2,8,9–Tetraazadispiro[4.1.4.2]tride-ca–2,9–dien–6–ones – Regioselectivesynthetic approaches towards 1,2,8,9–

tetraazadispiro[4.1.4.2]trideca–2,9–dien–6–ones of potential antimicrobial proper-ties, 2447

1,2–Benzothiazine–3–carbohydrazide1,1–dioxides – A facile synthesis of novelbiologically active 4–hydroxy–N'–(benzyli-dene)–2H–benzo[e][1,2]thiazine–3–carbo-hydrazide 1,1–dioxides, 1311

1,2–Oxazines – Synthesis of new series of5,6–dihydro–4H–1,2–oxazines via heteroDiels–Alder reaction and evaluation ofantimicrobial activity, 280

1,3,4–Oxadiazin–5(6H)–ones – Novel4H–1,3,4–oxadiazin–5(6H)–ones withhydrophobic and long alkyl chains: Design,synthesis, and bioactive diversity on inhibi-tion of monoamine oxidase, chitin biosyn-thesis and tumor cell, 2113

1,3,4–Oxadiazole – Synthesis of some new1,2,4–triazoles, their Mannich and Schiffbases and evaluation of their antimicrobialactivities, 1057 – A new type of five–mem-bered heterocyclic inhibitors of basic metal-locarboxypeptidases, 3266 – Fenbufenbased 3–[5–(substituted aryl)–1,3,4–oxadia-zol–2–yl]–1–(biphenyl–4–yl)propan–1–ones as safer antiinflammatory and analgesicagents, 3798 – Synthesis and pharmacolog-ical evaluation of 1,3,4–oxadiazole bearingbis(heterocycle) derivatives as anti–inflam-matory and analgesic agents, 3898 –Synthesis, physicochemical properties andantimicrobial activity of some new benzim-idazole derivatives, 4028 – Synthesis ofsome new 1,2,4–triazoles starting fromisonicotinic acid hydrazide and evaluationof their antimicrobial activities, 4362

1,3,4–Oxadiazole/thiadiazoles – Synthesisand antibacterial activity of some novelbis–1,2,4–triazolo[3,4–b]–1,3,4–thiadia-zoles and bis–4–thiazolidinone derivativesfrom terephthalic dihydrazide, 5112

1,3,4–Oxadiazoles – Synthesis, antimicrobialand cytotoxic activities of 1,3,4–oxadia-zoles, 1,3,4–thiadiazoles and 1,2,4–tria-zoles, 2106 – Synthesis and bioassay of anew class of heterocycles pyrrolyl oxadia-zoles/thiadiazoles/triazoles, 2313 –Aroylpropionic acid based 2,5–disubstitut-ed–1,3,4–oxadiazoles: Synthesis and theiranti–inflammatory and analgesic activities,2372

1,3,4–thiadiazines – Synthesis and antitumoractivity studies of some new fused 1,2,4–tri-azole derivatives carrying 2,4–dichloro–5–fluorophenyl moiety, 5066

1,3,4–Thiadiazole – Synthesis of some new1,2,4–triazoles, their Mannich and Schiffbases and evaluation of their antimicrobial

Keyword index

doi:10.1016/S0223-5234(09)00568-6

Available online at www.sciencedirect.com

http://www.elsevier.com/locate/ejmech

Page 2: Chal Micro

5132 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

activities, 1057 – Synthesis and antibacteri-al activity of nitroaryl thiadiazole–gati-floxacin hybrids, 1205 –Nitroimidazolyl–1,3,4–thiadiazole–basedanti–leishmanial agents: Synthesis and invitro biological evaluation, 1758 –Synthesis, antifungal activities and3D–QSAR study of N–(5–substitut-ed–1,3,4–thiadiazol–2–yl)cyclopropanecar-boxamides, 2782 – Synthesis of some new1,3,4–thiadiazol–2–ylmethyl–1,2,4–triazolederivatives and investigation of theirantimicrobial activities, 2896

1,3,4–Thiadiazoles – Synthesis, cytotoxicityand effects of some 1,2,4–triazole and1,3,4–thiadiazole derivatives on immuno-competent cells, 63 – Synthesis, antimicro-bial and cytotoxic activities of 1,3,4–oxadi-azoles, 1,3,4–thiadiazoles and 1,2,4–tria-zoles, 2106 – Synthesis and bioassay of anew class of heterocycles pyrrolyl oxadia-zoles/thiadiazoles/triazoles, 2313 –Synthesis of new chiral 2,5–disubstituted1,3,4–thiadiazoles possessing �–butenolidemoiety and preliminary evaluation of invitro anticancer activity, 3340

1,3,5–Triazine – Synthesis and antileishma-nial activity of novel 2,4,6–trisubstitutedpyrimidines and 1,3,5–triazines, 2473

1,3–Dibenzyl urea – Rare dipeptide and ureaderivatives from roots of Moringa oleiferaas potential anti–inflammatory andantinociceptive agents, 432

1,3–Dipolar cycloaddition – Synthesis and invivo antidiabetic activity of noveldispiropyrrolidines through [3�2] cycload-dition reactions with thiazolidinedione andrhodanine derivatives, 3272 – A facile syn-thesis and antimycobacterial evaluation ofnovel spiro–pyrido–pyrrolizines and pyrro-lidines, 3821

1,3–Dipolar cycloaddition reactions –Regioselective synthetic approachestowards 1,2,8,9–tetraazadispiro[4.1.4.2]trideca–2,9–dien–6–ones of potentialantimicrobial properties, 2447

1,3–Disubstituted ��–carboline derivatives –Synthesis and antiviral activity of ��–car-boline derivatives bearing a substituted car-bohydrazide at C–3 against poliovirus andherpes simplex virus (HSV–1), 4695

1,4,7,10–Tetraazacyclododecane (cyclen) –Hydrolytic cleavage of DNA by urea–bridged macrocyclic polyamines, 5090

1,4–Diazepanes – 1,4–Diazepanes derivedfrom (S)–serine – Homopiperazines withimproved �1 (sigma) receptor affinity andselectivity, 519

1,4–Dihydropyridine–3,5–dicarbamoxam-ide derivatives – Synthesis and antituber-cular activity of novel 4–substituted imida-zolyl–2,6–dimethyl–N3,N5–bisaryl–1,4–dihydropyridine–3,5–dicarboxamides, 3253

1,4–Naphthoquinone derivatives –2,3–Disubstituted–1,4–naphthoquinones,12H–benzo[b]phenothiazine–6,11–dionesand related compounds: Synthesis andBiological evaluation as potential antiprolif-erative and antifungal agents, 1086

1,5–Benzothiazepine – Synthesis and biolog-ical evaluation of a novel series of 1,5–ben-

zothiazepine derivatives as potential antimi-crobial agents, 2815

1,5–Diarylpyrazolin–3–one – Design, syn-thesis and pharmacological screening ofnovel nitric oxide donors containing1,5–diarylpyrazolin–3–one as nontoxicNSAIDs, 4622

1,5–Diarylpyrroles – 1,5–Diaryl–2–ethylpyrrole derivatives as antimycobacterialagents: Design, synthesis, and microbiolog-ical evaluation, 4734

1,8–Naphthyridine – 1,8–Naphthyridine–3–carboxamide derivatives with anticancerand anti–inflammatory activity, 3356

11��–HSD1 – Structure–based virtual screen-ing for identification of novel 11�–HSD1inhibitors, 1167

11��–HSD2 – Structure–based virtual screen-ing for identification of novel 11�–HSD1inhibitors, 1167

13C CP/MAS NMR – Novel 3,3'–diindolyl-methane derivatives: Synthesis and cytotox-icity, structural characterization in solidstate, 4136

13C NMR – The structure of Rimonabant inthe solid state and in solution: An experi-mental and theoretical study, 1864

13–cis–Retinoic acid – Synthesis, characteri-zation and in vitro antiproliferative activi-ties of new 13–cis–retinoyl ferrocene deriv-atives, 2572

14��–Demethylase – Design, synthesis, andantifungal activity of triazole and benzotria-zole derivatives, 3064

15N NMR – The structure of Rimonabant inthe solid state and in solution: An experi-mental and theoretical study, 1864

15–Membered macrolide analogs –Synthesis and antibacterial activity of novel15–membered macrolide derivatives:4"–Carbamate, 11,12–cyclic carbon-ate–4"–carbamate and 11,4"–di–O–arylcar-bamoyl analogs of azithromycin, 4010

17��–Hydroxylase–17,20–lyase (CYP17)inhibitors – Novel CYP17 inhibitors:Synthesis, biological evaluation, structure–activity relationships and modelling ofmethoxy– and hydroxy–substituted methyl-eneimidazolyl biphenyls, 2765

1H NMR – The structure of Rimonabant in thesolid state and in solution: An experimentaland theoretical study, 1864

1H–Benzimidazole derivatives – Synthesisand biological activity evaluation of 1H–ben-zimidazoles via mammalian DNA topoiso-merase I and cytostaticity assays, 2280

1H–Indazole–1–carboxamides – Synthesisand antiproliferative activity of 3–amino–N–phenyl–1H–indazole–1–carboxamides,165

1–[2–Thiazol–5–yl–(2–aminoethyl)]–4–n–propylpiperazine derivatives – Non–imida-zole histamine H3 ligands, Part IV: SAR of1–[2–thiazol–5–yl–(2–aminoethyl)]–4–n–propylpiperazine derivatives, 1674

1–Benzhydrylpiperazine derivatives –Synthesis and in vitro antiproliferative activ-ity of novel 1–benzhydrylpiperazine deriva-tives against human cancer cell lines, 1223

1–Halogenated benzyl–7–chloro–6–hydroxy–tetrahydroisoquinolines –

Structure–activity relationship of dopamin-ergic halogenated 1–benzyl–tetrahydroiso-quinoline derivatives, 4616

1–Hydroxy–6–(2–(1–piperidinyl)ethoxy)xanthone – Synthesis and characterization ofthe Zn(II) and Cu(II) piperidinyl isoeuxan-thone complexes: DNA–binding and cyto-toxic activity, 4509

2(3H)–Benzothiazolones – Synthesis andantioxidant potential of novel synthetic ben-zophenone analogues, 2724

2,3–Dichloro–1,4–naphthoquinone –Design, synthesis and biological evaluationof novel nitrogen and sulfur containing het-ero–1,4–naphthoquinones as potent antifun-gal and antibacterial agents, 3130

2,3–Dimethoxy–3–hydroxy–2–(1–phenyl–3–aryl–4–pyrazolyl)chromanones – Synthesisand antibacterial activity of some new2,3–dimethoxy–3–hydroxy–2–(1–phenyl–3–aryl–4–pyrazolyl)chromanones, 1763

2,4–dichloro–5–fluorophenyl – Synthesisand antitumor activity studies of some newfused 1,2,4–triazole derivatives carrying2,4–dichloro–5–fluorophenyl moiety, 5066

2,4–Imidazolidinediones – Synthesis and invitro anticancer activity of 2,4–azolidine-dione–acetic acids derivatives, 3627

2,4–Thiazolidinediones – Synthesis and invitro anticancer activity of 2,4–azolidine-dione–acetic acids derivatives, 3627

2,5–Bis(arylmethylidene)cyclopentanones –Regioselective synthetic approachestowards 1,2,8,9–tetraazadispiro[4.1.4.2]trideca–2,9–dien–6–ones of potentialantimicrobial properties, 2447

2,6–Diarylpiperidin–4–one – Synthesis,spectral and biological evaluation of somenew thiazolidinones and thiazoles based ont–3–alkyl–r–2,c–6–diarylpiperidin–4–ones,4199

25Mg2��–magnetic isotope effect – The por-phyrin–fullerene nanoparticles to promotethe ATP overproduction in myocardium:25Mg2�–magnetic isotope effect, 1554

2D 1H 13C NMR spectra of ingenol esters –Bio–active compounds from Euphorbiacornigera Boiss, 3188

2D molecular descriptors – Classificationmodels for CYP450 3A4 inhibitors andnon–inhibitors, 2354

2D NMR – Synthesis, characterization andantimicrobial activity of Co(II), Zn(II) andCd(II) complexes with N–benzyloxycar-bonyl–S–phenylalanine, 1537

2D nuclear Overhauser enhancement spec-troscopy – Studies on self–aggregation ofanthracycline drugs by restrained moleculardynamics approach using nuclear magneticresonance spectroscopy supported byabsorption, fluorescence, diffusion orderedspectroscopy and mass spectrometry, 1437

2D–QSAR – Synthesis, biological evaluationand 2D–QSAR analysis of benzoxazoles asantimicrobial agents, 501 – QSAR studiesfor diarylpyrimidines against HIV–1reverse transcriptase wild–type and mutantstrains, 625 – Novel 4–(morpholin–4–yl)–N'–(arylidene)benzohydrazides:Synthesis, antimycobacterial activity andQSAR investigations, 3954

Page 3: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5133

2H–Benzimidazole 1,3–dioxide – Secondgeneration of 2H–benzimidazole 1,3–diox-ide derivatives as anti–trypanosomatidagents: Synthesis, biological evaluation,and mode of action studies, 4426

2–(Arylmethylene)–2,3–dihydro–1H–inden–1–ones – Regioselective synthesis ofd i s p i r o [ 1 H – i n d e n e – 2 , 3 ' – p y r r o l i -dine–2',3"–[3H]indole]–1,2"(1"H)–dionesof potential anti–tumor properties, 91

2–[(Substituted amino)thiocarbonyl]cyano-acetohydrazides – Synthesis of [1,2,4]tria-zolo[1,5–a]pyridines of potential PGE2inhibitory properties, 1972

2–[1–(5–Chloro–2–methoxy–phenyl)–5–methyl–1H–pyrazol–4–yl]–5–(substituted–phenyl)–[1,3,4]oxadiazoles – Synthesis,characterization and antibacterial activity of2–[1–(5–chloro–2–methoxy–phenyl)–5–methyl–1H–pyrazol–4–yl]–5–(substituted–phenyl)–[1,3,4]oxadiazoles, 4522

2–Acetyl–2–ethoxycarbonyl–1–[4(4'–aryla-zo)–phenyl]–N,N–dimethylaminophenylaziridines – Synthesis and QSAR modelingof 2–acetyl–2–ethoxycarbonyl–1–[4(4 '–arylazo)–phenyl]–N ,N–dimethy-laminophenyl aziridines as potential anti-bacterial agents, 251

2–Acetylnaphthalene – Synthesis andanti–tumor activities of some new pyridinesand pyrazolo[1,5–a]pyrimidines, 3519

2–Acylhydrazino–5–arylpyrroles –2–Acylhydrazino–5–arylpyrrole deriva-tives: Synthesis and antifungal activity eval-uation, 1288

2–Aminobenzothiazoles – Synthesis and anti-tumor activity of optically active thioureaand their 2–aminobenzothiazole deriva-tives: A novel class of anticancer agents,2923

2–Amino–1,3,4–thiadiazole – Synthesis andantimicrobial studies of novel methylenebridged benzisoxazolyl imidazo[2,1–b][1,3,4]thiadiazole derivatives, 2828

2–Amino–4H–pyrans – A facile one–potgreen synthesis and antibacterial activity of2–amino–4H–pyrans and 2–amino–5–oxo–5,6,7,8–tetrahydro–4H–chromenes, 3805

2–Amino–benzo[d]isothiazol–3–one deriva-tives – Hybrid molecules between benzene-sulfonamides and active antimicrobialbenzo[d]isothiazol–3–ones, 2741

2–Aminophenol – Biological activity studieson metal complexes of novel tridentateSchiff base ligand. Spectroscopic and ther-mal characterization, 4801

2–Arachidonoylglycerol – The synthesis andbiological evaluation of para–substitutedphenolic N–alkyl carbamates as endo-cannabinoid hydrolyzing enzyme inhibitors,2994

2–Aryl–naphtho[1,2–d]oxazole – Novel2–aryl–naphtho[1,2–d]oxazole derivativesas potential PTP–1B inhibitors showingantihyperglycemic activities, 109

2–Azaspiro[4.5]decane–1,3–dione – Theinfluence of an ethylene spacer on the5–HT1A and 5–HT2A receptor affinity ofarylpiperazine derivatives of amides withN–acylated amino acids and 3–differentlysubstituted pyrrolidine–2,5–diones, 800

2–Azetidinone derivatives – 2–Azetidinonederivatives: Design, synthesis and evalua-tion of cholesterol absorption inhibitors,1638

2–Azetidinone – 2–Azetidinone derivatives:Design, synthesis, in vitro anti–microbial,cytotoxic activities and DNA cleavagestudy, 5123

2–Benzimidazoles – Synthesis and evaluationof some new benzimidazole derivatives aspotential antimicrobial agents, 2294

2–Benzylsulfanyl derivatives – Preparationand in vitro evaluation of benzylsulfanylbenzoxazole derivatives as potential antitu-berculosis agents, 2286

2–Chloro–5–methylpyridine–3–olefinderivatives – Synthesis, photochemical E(trans)�Z (cis) isomerization and antimi-crobial activity of 2–chloro–5–methylpyri-dine–3–olefin derivatives, 4661

2–Chloro–N6–substituted–4"–thioadeno-sine–5'–uronamide derivatives as humanA3 receptor ligands – Topological descrip-tors in modeling the agonistic activity ofhuman A3 adenosine receptor ligands: Thederivatives of 2–chloro–N6–substituted–4'–thioadenosine–5’–uronamide, 1377

2–Cyanopyrrolidine – Synthesis and evalua-tion of structurally constrained imidazolidinderivatives as potent dipeptidyl peptidaseIV inhibitors, 3318

2–Deacetoxytaxinine J (2–DAT–J) – In vitroand in vivo anticancer activity of 2–deace-toxytaxinine J and synthesis of novel tax-oids and their in vitro anticancer activity,3947

2–Methylbenzimidazole – New transitionmetal ion complexes with benzimida-zole–5–carboxylic acid hydrazides withantitumor activity, 1500

2 – O x o – q u i n o l i n e – 3 – c a r b a l d e h y d eSchiff–bases – Synthesis, crystal structure,DNA interaction and antioxidant activitiesof two novel water–soluble Cu(2�) com-plexes derivated from2 – o x o – q u i n o l i n e – 3 – c a r b a l d e h y d eSchiff–bases, 4477

2–PAM – In–vitro regeneration of sarin inhib-ited electric eel acetylcholinesterase bybis–pyridinium oximes bearing xylene link-er, 1326 – Synthesis and evaluation of novelbis–pyridinium oximes as reactivators ofDFP–inhibited acetylcholinesterase, 1335

2–Phenylindole derivative – CoMFA anddocking studies of 2–phenylindole deriva-tives with anticancer activity, 2822

2–Pyrazoline – Synthesis and investigation ofanti–inflammatory activity and gastriculcerogenicity of novel nitric oxide–donat-ing pyrazoline derivatives, 3068

2–Styrylchromone – Synthesis of2–styrylchromones as a novel class ofantiproliferative agents targeting carcinomacells, 2552

2–Substituted benzimidazoles – Convenientone–pot synthesis of novel 2–substituted ben-zimidazoles, tetrahydrobenzimidazoles andimidazoles and evaluation of their in vitroantibacterial and antifungal activities, 1751

2–Thieno–4(3H)–quinazolinones –Substituted quinazolines, part 3. Synthesis,

in vitro antitumor activity and molecularmodeling study of certain2–thieno–4(3H)–quinazolinone analogs,2379

2–Thioxo–quinazoline – S– and C–nucleosi-doquinazoline as new nucleoside analogswith potential analgesic and anti–inflamma-tory activity, 4249

2–Thioxopyrimido[4,5–b]quinoline – Newacyclic nucleosides analogues as potentialanalgesic, anti–inflammatory, anti–oxidantand anti–microbial derived from pyrimi-do[4,5–b]quinolines, 1427

2’–C–Methylcytidine – Cyclic phosphorami-dates as prodrugs of 2’–C–methylcytidine,3765

3,1–Benzoxazine – Convenient synthesis andantimicrobial evaluation of some novel2–substituted–3–methylbenzofuran deriva-tives, 3637

3,3–Diphenylalanine enantiomers –Arginine vasopressin and its analogues –The influence of position 2 modificationwith 3,3–diphenylalanine enantiomers.Highly potent V2 agonists, 2862

3,3–Diphenylpyrrolidin–2–one derivatives– Design, synthesis and pharmacologicalevaluation of new 1–[3–(4–arylpiper-azin–1–yl)–2–hydroxy–propyl]–3,3–diphenylpyrrolidin–2–one derivatives with antiar-rhythmic, antihypertensive, and�–adrenolytic activity, 3994

3,3'–Dindolylmethane derivatives – Novel3,3'–diindolylmethane derivatives:Synthesis and cytotoxicity, structural char-acterization in solid state, 4136

3,4–Dihydro–3–oxo–2H–benzo[b][1,4]oxazine – Synthesis of 2–(4–substituted-methylpiperazin–1–yl)–N–(3,4–dihy-dro–3–oxo–2H–benzo[b][1,4]oxazin–7–yl)acetamides and their positive inotropic eval-uation, 3027

3,5–Bis(arylmethylene)–1–methyl–4–piperidinones – Regioselective synthesis andstereochemical structure of anti–tumoractive dispiro[3H–indole–3,2'–pyrroli-dine–3',3"–piperidine]–2(1H),4"–diones,1257

3D QSAR – Synthesis, evaluation and 3DQSAR analysis of novel estradiol–RGDoctapeptide conjugates with oral anti–osteo-porosis activity, 1689 – Application of 3DQSAR CoMFA/CoMSIA and in silico dock-ing studies on novel renin inhibitors againstcardiovascular diseases, 3703 – NovelN–(3–carboxyl–9–benzyl–�–carboline–1–yl)ethylamino acids: Synthesis, anti–tumorevaluation, intercalating determination, 3DQSAR analysis and docking investigation,4153 – Novel Biginelli dihydropyrimidineswith potential anticancer activity: A parallelsynthesis and CoMSIA study, 4192 – 3DQSAR study of the toxicity of trichothecenemycotoxins, 4485 – A class of novelN–(3S–1,2,3,4–tetrahydroisoquinoline–3–carbonyl)–l–amino acid derivatives: theirsynthesis, anti–thrombotic activity evalua-tion, and 3D QSAR analysis, 4904

3D–QSAR CoMFA/CoMSIA – 3D–QSARCoMFA/CoMSIA models based on theoret-ical active conformers ofHOE/BAY–793

Page 4: Chal Micro

5134 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

analogs derived from HIV–1 proteaseinhibitor complexes, 4344

3D–QSAR – Docking, 3D–QSAR studies andin silico ADME prediction on c–Src tyro-sine kinase inhibitors, 990 – Predictinganti–HIV activity of 1,3,4–thiazolidinonederivatives: 3D–QSAR approach, 1180 –Receptor–based 3D–QSAR studies ofcheckpoint Wee1 kinase inhibitors, 1383 –2D– and 3D–QSAR of Tocainide andMexiletine analogues acting as Nav1.4channel blockers, 1477 – 3D–QSAR studiesof boron–containing dipeptides as protea-some inhibitors with CoMFA and CoMSIAmethods, 1486 – GRIND–based 3D–QSARand CoMFA to investigate topics dominatedby hydrophobic interactions: The case ofhERG K� channel blockers, 1926 –Thiocarbamates as non–nucleoside HIV–1reverse transcriptase inhibitors:Docking–based CoMFA and CoMSIAanalyses, 2059 – Development of CoMFAand CoMSIA models of affinity and selec-tivity for indole ligands of cannabinoid CB1and CB2 receptors, 2482 – Synthesis, anti-fungal activities and 3D–QSAR study ofN–(5–substituted–1,3,4–thiadiazol–2–yl)cyclopropanecarboxamides, 2782 –3D–QSAR studies of HDACs inhibitorsusing pharmacophore–based alignment,2868 – 3D–QSAR studies on the inhibitorsof AP–1 and NF–�B mediated transcrip-tional activation, 2888 – CoMFA, LeapFrogand blind docking studies on sulfonanilidederivatives acting as selective aromataseexpression regulators, 3445 – Docking and3D–QSAR studies of BMS–806 analogs asHIV–1 gp120 entry inhibitors, 3524 –Discovery of potential new InhA directinhibitors based on pharmacophoreand3D–QSAR analysis followed by in silicoscreening, 3718 – Novel4–(morpholin–4–yl)–N'–(arylidene)benzo-hydrazides: Synthesis, antimycobacterialactivity and QSAR investigations, 3954 –3D–QSAR with the aid of pharmacophoresearch and docking–based alignments forfarnesyltransferase inhibitors, 4070 – Selforganizing molecular field analysis on aseries of human 5�–reductase inhibitors:Unsaturated 3–carboxysteroid, 4920

3–(2,4–Dichloro–5–fluorophenyl)–4H–1,2,4–triazole–5–thiol – Synthesis, analgesic,anti–inflammatory and antimicrobial stud-ies of 2,4–dichloro–5–fluorophenyl con-taining thiazolotriazoles, 827

3–(2–Methylphenyl)–pyrrolidine–2,5–dione– Synthesis and anticonvulsant activity ofnew N–[(4–arylpiperazin–1–yl)–alkyl]derivatives of 3–phenyl–pyrrolidine–2,5–dione, 2224

3–(2–Trifluoromethylphenyl)–pyrroli-dine–2,5–dione – Synthesis and anticon-vulsant activity of new N–[(4–arylpiper-azin–1–yl)–alkyl] derivatives of3–phenyl–pyrrolidine–2,5–dione, 2224

3–Aminobenzo[d]isothiazole derivatives –Evaluation of the local anaesthetic activityof 3–aminobenzo[d]isothiazole derivativesusing the rat sciatic nerve model, 473

3–Amino–2–hydroxypropoxyisoflavone –Synthesis and anti–osteoporotic evaluation

of certain 3–amino–2–hydroxypropoxy-isoflavone derivatives, 3621

3–Aminopyrazols – Synthesis and anti–tumoractivities of some new pyridines and pyra-zolo[1,5–a]pyrimidines, 3519

3–Aroyl–2,3–dihydro–1,1–dioxo–1,4,2–ben-zodithiazines – Synthesis and anti–HIV–1integrase activities of 3–aroyl–2,3–dihy-dro–1,1–dioxo–1,4,2–benzodithiazines, 190

3–Hydroxy–2–(1–phenyl–3–aryl–4–pyra-zolyl)chromones – Synthesis and antibac-terial activity of some new2,3–dimethoxy–3–hydroxy–2–(1–phenyl–3–aryl–4–pyrazolyl)chromanones, 1763

3–Hydroxypropylamides – The novel phos-phoramidate derivatives of NSAID3–hydroxypropylamides: Synthesis, cyto-static and antiviral activity evaluations, 143

3–Hydroxypyran–4–ones – Synthesis,antimicrobial evaluation and QSAR studyof some 3–hydroxypyridine–4–one and3–hydroxypyran–4–one derivatives, 2145

3–Hydroxypyridin–4–ones – Synthesis,antimicrobial evaluation and QSARstudy of some 3–hydroxypyridine–4–one and 3–hydroxypyran–4–onederivatives, 2145

3–Iminoindolin–2–ones – Synthesis andantimicrobial activity of new 1–alkyl/cyclo-hexyl–3,3–diaryl–1'–methylspiro[azeti-dine–2,3'–indoline]–2',4–diones, 2265

3–Mercaptopropionic acid – Design and syn-thesis of 5–alkoxy–[1,2,4]triazolo[4,3–a]quinoline derivatives with anticon-vulsant activity, 954 – Design, synthesis of8–alkoxy–5,6–dihydro–[1,2,4]triazino[4,3–a]quinolin–1–ones with anticonvulsantactivity, 1265

4(3H)–Quinazolinones – Synthesis, anticon-vulsant and CNS depressant activity ofsome new bioactive 1–(4–substituted–phenyl)–3–(4–oxo–2–phenyl/ethyl–4H–quinazolin–3–yl)–urea, 4335

4,5–Dihydroxypyrimidine carboxamides –Multivariate QSAR study of 4,5–dihydrox-ypyrimidine carboxamides as HIV–1 inte-grase inhibitors, 3577

4,5–Diphenyloxazolone – Synthesis and bio-logical evaluation of 4,5–diphenyloxa-zolone derivatives on route towards selec-tive COX–2 inhibitors, 1830

4,5–Disubstituted acridine – Synthesis andbiological evaluation of novel4,5–bis(dialkylaminoalkyl)–substitutedacridines as potent telomeric G–quadruplexligands, 3880

4–Amino derivatives – Design and synthesisof azolopyrimidoquinolines, pyrimido-quinazolines as anti–oxidant, anti–inflam-matory and analgesic activities, 609

4–Aminoantipyrine – Biological activitystudies on metal complexes of novel triden-tate Schiff base ligand. Spectroscopic andthermal characterization, 4801

4–Aminobicyclo[2.2.2]octane derivative –Antiplasmodial and antitrypanosomal activ-ities of aminobicyclo[2.2.2]octyl�–aminoalkanoates, 736

4–Aminosalicylic acid – Colon–specificmutual amide prodrugs of 4–aminosalicylicacid for their mitigating effect on experi-mental colitis in rats, 131

4–Anilinoquinazoline – Synthesis and in vitroantitumor activities of novel 4–anilino-quinazoline derivatives, 3046 – Synthesisand characterization of rhenium and tech-netium–99m tricarbonyl complexes bearingthe 4–[3–bromophenyl]quinazoline moietyas a biomarker for EGFR–TK imaging,4021

4–Arylpiperazine derivatives – Synthesisand anticonvulsant activity of newN–[(4–arylpiperazin–1–yl)–alkyl] deriva-tives of 3–phenyl–pyrrolidine–2,5–dione,2224

4–Hydroxycoumarins – Investigation of theantioxidant properties of some new4–hydroxycoumarin derivatives, 3077

4–Isopropylthiazole–2–carbohydrazideanalogs – Synthesis of new 4–isopropylthi-azole hydrazide analogs and some derivedclubbed triazole, oxadiazole ring systems –A novel class of potential antibacterial, anti-fungal and antitubercular agents, 4739

4–MTA – Synthesis and serotonin transporteractivity of sulphur–substituted �–alkylphenethylamines as a new class of anti-cancer agents, 4862

4–Nitroimidazoles – Synthesis and in vitrotrichomonicidal, giardicidal and amebicidalactivity ofN–acetamide(sulfonamide)–2–methyl–4–nitro–1H–imidazoles, 2975

4–Oxy/thio substituted–1H–pyrazol–5(4H)–ones – Synthesis of some novelbioactive 4–oxy/thio substituted–1H–pyra-zol–5(4H)–ones via efficient cross–Claisencondensation, 3852

4–Phenyl–but–3–en–2–one – Analgesic, anti-convulsant and anti–inflammatory activitiesof some synthesized benzodiazipine, tria-zolopyrimidine and bis–imide derivatives,4787

4–Piperidones – The cytotoxic properties andpreferential toxicity to tumour cells dis-played by some 2,4–bis(benzylidene)–8 – m e t h y l – 8 – a z a b i c y c l o [ 3 . 2 . 1 ]octan–3–ones and 3,5–bis(benzyli-dene)–1–methyl–4–piperidones, 54

4–Substituted–1,2,4–triazole–3–thiones –Synthesis, characterization and antibacterialactivity of some triazole Mannich bases car-rying diphenylsulfone moieties, 3083

4–Thiazolidinones – Synthesis, characteriza-tion and in vitro antimicrobial activity ofnovel 2–thioxo–4–thiazolidinones and4,4'–bis(2–thioxo–4–thiazolidinone–3–yl)diphenylsulfones, 4148

4–Thioxothiazolidinones – Synthesis, antimi-crobial and cytotoxic activities of some5–arylidene–4–thioxo–thiazolidine–2–ones,2038

4'–Epiadriamycin, adriamycin and dauno-mycin – Studies on self–aggregation ofanthracycline drugs by restrained moleculardynamics approach using nuclear magneticresonance spectroscopy supported byabsorption, fluorescence, diffusion orderedspectroscopy and mass spectrometry, 1437

5,7–Diamino–3–phenyl–2–benzylamino,2–phenoxy and 2–phenylthio substitutedquinoxalines – Synthesis and in vitro anti-tumor activity of new quinoxaline deriva-tives, 1579

Page 5: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5135

5H–Dibenzo[c,h][1,6]naphthyridin–6–ones– Cytotoxicity and TOP1–targeting activityof 8– and 9–amino derivatives of 5–butyl–and 5–(2–N,N–dimethylamino)e t h y l – 5 H – d i b e n z o [ c , h ] [ 1 , 6 ] n a p h -thyridin–6–ones, 1471 – Novel topoiso-merase I–targeting antitumor agents synthe-sized from the N,N,N–trimethylammoniumderivative of ARC–111, 5H–2,3–dimethoxy–8,9–methylenedioxy–5–[(2–N,N,N–trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin–6–one iodide, 3433

5–(4–Methyl–1,2,3–triazole)methyl oxazo-lidinone – Synthesis and antibacterial activ-ity of novel 5–(4–methyl–1H–1,2,3–tria-zole) methyl oxazolidinones, 3217

5–Amino–1,10–phenanthroline –Antitumour activity of novel 1,10–phenan-throline and 5–amino–1,10–phenanthrolinederivatives, 2720

5–Amino–6,8–dicyano–1H–[1,2,4]triazo-lo[1,5–a]pyridines – Synthesis of[1,2,4]triazolo[1,5–a]pyridines of potentialPGE2 inhibitory properties, 1972

5–Aminosalicylic acid – Synthesis, kineticstudies and pharmacological evaluation ofmutual azo prodrugs of 5–aminosalicylicacid for colon–specific drug delivery ininflammatory bowel disease, 3922

5–Benzylidene barbiturate – Inhibitoryeffects of 5–benzylidene barbiturate deriva-tives on mushroom tyrosinase and theirantibacterial activities, 4235

5–HT system connection – Synthesis, phar-macological and antiviral activity of1,3–thiazepine derivatives, 4960

5–HT1A receptor – Synthesis and serotoninreceptor activity of the arylpiperazinealkyl/propoxy derivatives of new azatricy-cloundecanes, 152

5–HT1A, 5–HT2A, D1, D2 receptor affinities –Synthesis and preliminary pharmacologicalevaluation of imidazo[2,1–f]purine–2,4–dione derivatives, 4288

5–HT1A/5–HT2A receptor ligands – Theinfluence of an ethylene spacer on the5–HT1A and 5–HT2A receptor affinity ofarylpiperazine derivatives of amides withN–acylated amino acids and 3–differentlysubstituted pyrrolidine–2,5–diones, 800

5–HT1A/5–HT–T dual activity – Novel4–aryl–pyrido[1,2–c]pyrimidines with dualSSRI and 5–HT1A activity, Part 1, 1710

5–HT2A receptor – Synthesis and serotoninreceptor activity of the arylpiperazinealkyl/propoxy derivatives of new azatricy-cloundecanes, 152

5–HT3 receptor – Molecular properties ofpsychopharmacological drugs determiningnon–competitive inhibition of 5–HT3Areceptors, 2667

5–HT4 ligands – Synthesis and preliminaryscreening of novel indole–3–methanaminesas 5–HT4 receptor ligands, 2952

5–HT4 receptor model – Synthesis and prelimi-nary screening of novel indole–3–methanaminesas 5–HT4 receptor ligands, 2952

5–Lipoxygenase – New pyridone, thioxopyri-dine, pyrazolopyridine and pyridine deriva-tives that modulate inflammatory mediatorsin stimulated RAW 264.7 murinemacrophage, 4547

5–Nitrofuranes – 5–Nitro–2–furyl derivativeactives against Trypanosoma cruzi:Preliminary in vivo studies, 3909

5–Nitrofuryl containing thiosemicar-bazones – Effect of ruthenium complexa-tion on trypanocidal activity of 5–nitrofurylcontaining thiosemicarbazones, 4937

5–Nitroimidazoles – Lowering of 5–nitroimi-dazole’s mutagenicity: Towards optimalantiparasitic pharmacophore, 653

5–Nitroindazole – Study of 5–nitroindazoles’anti–Trypanosoma cruzi mode of action:Electrochemical behaviour and ESR spec-troscopic studies, 1545

5–Substituted–1,2,4–triazole–3–thiole –Synthesis, characterization and evaluationof antibacterial activity of some thiazo-lo[3,2–b][1,2,4]triazole incorporatingdiphenylsulfone moieties, 4752

6Hz test – A new class of anticonvulsants pos-sessing 6Hz activity: 3,4–Dialkyloxy thio-phene bishydrazones, 4376

6–Heteroaryl tricyclic analogues – Synthesisand anti–VZV activity of 6–heteroaryl deriv-atives of tricyclic acyclovir and9–{[cis–1',2'–bis(hydroxymethyl)cyclo-prop–1'–yl]methyl}guanine analogues, 3313

6–Mercaptopurine – Novel derivatives of6–mercaptopurine: Synthesis, characteriza-tion and antiproliferative activities ofS–allylthio–mercaptopurines, 541 –Captopril and 6–mercaptopurine: Whose SHpossesses higher antioxidant ability?, 4841

6–Pyridone – Design and synthesis of calpaininhibitory 6–pyridone 2–carboxamidederivatives, 1331

7 – M e t h o x y c h ro m o n e – 3 – c a r b a l d e -hyde–(4'–hydroxy) benzoyl hydrazone –Synthesis, crystal structure, antioxidantactivities and DNA–binding studies of theLn(III) complexes with 7–methoxy-chromone–3–carbaldehyde–(4'–hydroxy)benzoyl hydrazone, 2425

7–Methyljuglone – Juglone derivatives asantitubercular agents: A rationale for theactivity profile, 2847

8–(Trifluoromethyl)quinoline derivatives –Synthesis and antimicrobial activities ofnovel quinoline derivatives carrying1,2,4–triazole moiety, 4637

8–Aminoquinolines – Primaquine revisitedsix decades after its discovery, 937

8–Arylxanthines – Synthesis of a series of8–(substituted–phenyl)xanthines and astudy on the effects of substitution patternof phenyl substituents on affinity for adeno-sine A1 and A2A receptors, 2122

8–Hydroxyquinoline – Antidyslipidemic andantioxidative activities of 8–hydroxyquino-line derived novel keto–enamine Schiffsbases, 1813

9,10–Phenanthrenequinone diimine –Cytotoxic and genotoxic effects of[Ru(phi)3]

2� evaluated by Ames/Salmonellaand MTT methods, 2601

9–Anilinoacridines – Synthesis and in vitrocytotoxicity of 9–anilinoacridines bearingN–mustard residue on both anilino and acri-dine rings, 3056

[[1,2,4]–Triazole – SAR study of clubbed

[1,2,4]–triazolyl with fluorobenzimidazoles

as antimicrobial and antituberculosisagents, 2930

[1,2,4]Triazolo[3,4–d][1,3,4]thiadiazole –Synthesis and biological evaluation of3 , 6 – d i s u b s t i t u t e d[1,2,4]triazolo[3,4–b][1,3,4]thiadiazolederivatives as a novel class of potentialanti–tumor agents, 2776

[11C]FEDAA1106 – Synthesis of[11C]FEDAA1106 as a new PET imagingprobe of peripheral benzodiazepine receptorexpression, 2748

B��,�'–(EE)–Bis(benzylidene)–cycloalkanones

– A facile synthesis of ��,�'–(EE)–bis(ben-zylidene)–cycloalkanones and their antitu-bercular evaluations, 1705

AA1 and A2A adenosine receptors – Synthesis

of a series of 8–(substituted–phenyl)xan-thines and a study on the effects of substitu-tion pattern of phenyl substituents on affin-ity for adenosine A1 and A2A receptors,2122

B��1–, �2– and �1–Adrenoceptor antagonists –

Synthesis and adrenolytic activity of1–(1H–indol–4–yloxy)–3–(2–(2–methoxyphenoxy)ethylamino)propan–2–olanalogs and its enantiomers. Part 2, 5103

��1–, �2–, �1–Adrenoceptor antagonist –Synthesis and adrenolytic activity of1–(1H–indol–4–yloxy)–3–{[2–(2–methoxyphenoxy)ethyl]amino}propan–2–ol andits enantiomers. Part 1, 809

��1–Adrenoceptor blocking activity – The syn-thesis of N–phenoxyethyl–1–substitut-ed–1,2,3,4–tetrahydroisoquinolines andtheir ��1–adrenoceptor blocking activity,1271

AA431 and MCF–7 cell lines – Synthesis and

in vitro antitumor activities of novel 4–anili-noquinazoline derivatives, 3046

A549 cell line – 5–Benzylidene–hydantoins:Synthesis and antiproliferative activity onA549 lung cancer cell line, 3471

Ab initio – Computational study of the elec-tronic structure characterization of a novel-anti–inflammatory tripeptide derived frommonocyte locomotion inhibitoryfactor(MLIF)–pentapeptide, 3114

Ab initio – Mechanistic aspects of benzoth-iazepines: A class of antiarrhythmic drugs, 1

Ab initio reactivity – Large ring 1,3–bridged2–azetidinones: Experimental and theoreti-cal studies, 2071

Ab initio SCF, DFT – Molecular structure andstability of perindopril erbumine andperindopril l–arginine complexes, 101

ABCB1 – Identification of putativesteroid–binding sites in human ABCB1 andABCG2, 3601

ABCG2 – Identification of putativesteroid–binding sites in human ABCB1 andABCG2, 3601

Page 6: Chal Micro

5136 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Abietic acid – Synthesis and biological evalu-ation of abietic acid derivatives, 2468

Abl – Determination of permeability andlipophilicity of pyrazolo–pyrimidine tyro-sine kinase inhibitors and correlation withbiological data, 3712

Abraham equation – Prediction of convul-sant activity of gases and vapors, 885

Absorption model – Evaluation of substrateand inhibitor properties of a novel MDRmodulator H17 towards transmembraneefflux pumps, 3060

Abyssinone – Synthesis of (±)Abyssinone Iand related compounds: Their anti–oxidantand cytotoxic activities, 2239

ACE inhibitor – Molecular structure and sta-bility of perindopril erbumine and perindo-pril l–arginine complexes, 101

Acetanilide – Discovery of novel acetanilidederivatives as potent and selective�3–adrenergic receptor agonists, 2533

Acetylation – Preparation and antitubercularactivities in vitro and in vivo of novel Schiffbases of isoniazid, 4169

Acetylcholinesterase inhibitors – Synthesis,biological evaluation and molecular model-ing of oxoisoaporphine and oxoaporphinederivatives as new dual inhibitors of acetyl-cholinesterase/butyrylcholinesterase, 2523

Acetylcholinesterase – In–vitro regenerationof sarin inhibited electric eel acetyl-cholinesterase by bis–pyridinium oximesbearing xylene linker, 1326 – Synthesis andevaluation of novel bis–pyridinium oximesas reactivators of DFP–inhibited acetyl-cholinesterase, 1335 – New potential AChEinhibitor candidates, 3754

AChE inhibitors – Design, synthesis, andevaluation of benzophenone derivatives asnovel acetylcholinesterase inhibitors, 1341

AChE inhibitory activity – Design, synthesisand AChE inhibitory activity of indanoneand aurone derivatives, 7

AChE – Active site directed docking studies:Synthesis and pharmacological evaluation ofcis–2,6–dimethyl piperidine sulfonamides asinhibitors of acetylcholinesterase, 4057

Acid chloride – Synthesis of some novelbioactive 4–oxy/thio substituted–1H–pyra-zol–5(4H)–ones via efficient cross–Claisencondensation, 3852

Acidity – Computational study of the elec-tronic structure characterization of a novel-anti–inflammatory tripeptide derived frommonocyte locomotion inhibitoryfactor(MLIF)–pentapeptide, 3114

Acitretin – Preparation of spermine conju-gates with acidic retinoids with potentribonuclease P inhibitory activity, 2689

Acridine – Microwave–induced synthesis andanti–microbial activities of7,10,11,12–tetrahydrobenzo[c]acridin–8(9H)–one derivatives, 976 – Unusual cellularuptake of cytotoxic4–hydroxymethyl–3–aminoacridine, 4758

Acridines – Synthesis of new acridines andhydrazones derived from cyclic �–diketonefor cytotoxic and antiviral evaluation, 3680– Prediction of telomerase inhibitory activi-ty for acridinic derivatives based on chemi-cal structure, 4826

Acridones – Prediction of telomeraseinhibitory activity for acridinic derivativesbased on chemical structure, 4826

Actinonin derivatives – Design, synthesisand antibacterial activity of novel actinoninderivatives containing benzimidazole hete-rocycles, 2202

Activity – Molecular orbital differentiation ofagonist and antagonist activity in theGlycineB–iGluR–NMDA receptor, 2960

Acute toxicity – Synthesis, characterizationand antitumor activity of new type binuclearplatinum(II) complexes, 2322

Acyclic nucleoside phosphonates – Acyclicnucleoside bisphosphonates: Synthesis andproperties of chiral 2–amino–4,6–bis[(phos-phonomethoxy)alkoxy]pyrimidines, 2408

Acyclovir – Structure–activity relationshipsfor dipeptide prodrugs of acyclovir:Implications for prodrug design, 2339 –Synthesis and anti–VZV activity of 6–het-eroaryl derivatives of tricyclic acyclovir and9–{[cis–1',2'–bis(hydroxymethyl)cyclo-prop–1'–yl]methyl}guanine analogues, 3313

Acylation – Design, synthesis and molecularmodeling study of acylated 1,2,4–tria-zole–3–acetates with potential anti–inflam-matory activity, 117

Acylthiocarbamates – Parallel synthesis,molecular modelling and furtherstructure–activity relationship studies ofnew acylthiocarbamates as potentnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 2190

Acylthiosemicarbazide – Copper(II) anduranyl(II) complexes with acylthiosemicar-bazide: Synthesis, characterization, antibac-terial activity and effects on the growth ofpromyelocytic leukemia cells HL–60, 3323

Acylthioureas – N–Acylated and N,N'–diacy-lated imidazolidine–2–thione derivativesand N,N'–diacylated tetrahydropyrimi-dine–2(1H)–thione analogues: Synthesisand antiproliferative activity, 1106

Adamantane derivatives – Synthesis andanti–HIV studies of 2– and3 – a d a m a n t y l – s u b s t i t u t e dthiazolidin–4–ones, 303

Adamantane – Adamantane derivatives ofthiazolyl–N–substituted amide, as possiblenon–steroidal anti–inflammatory agents,1198

Adamantyl arotinoids – Highly twistedadamantyl arotinoids: Synthesis, antiprolif-erative effects and RXR transactivation pro-files, 2434

Adaptive neuro–fuzzy interference system –Quantitative structure–activity relationshipstudy of serotonin (5–HT7) receptorinhibitors using modified ant colony algo-rithm and adaptive neuro–fuzzy interfer-ence system (ANFIS), 1463

Adenine – Synthesis, characterization, antimi-crobial and antitumor screening of somediorganotin(IV) complexes of2–[(9H–Purin–6–ylimino)]–phenol, 3981

Adenosine – Synthesis of a series of N6–sub-stituted adenosines with activity against try-panosomatid parasites, 3665

Adenosine receptor antagonists – Synthesisof a series of 8–(substituted–phenyl)xan-

thines and a study on the effects of substitu-tion pattern of phenyl substituents on affin-ity for adenosine A1 and A2A receptors,2122

Adina cordifolia – Antiamoebic coumarinsfrom the root bark of Adina cordifolia andtheir new thiosemicarbazone derivatives,2252

ADME – Docking, 3D–QSAR studies and insilico ADME prediction on c–Src tyrosinekinase inhibitors, 990

ADME properties – Mapping the ribonucle-olytic active site of bovine seminal ribonu-clease. The binding of pyrimidinyl phos-phonucleotide inhibitors, 4496

Aggregation inhibitor – Synthesis and activ-ity of fibrillogenesis peptide inhibitors relat-ed to the 17–21 �–amyloid sequence, 179

Agonist – Discovery of novel acetanilidederivatives as potent and selective�3–adrenergic receptor agonists, 2533

Agonists – Molecular orbital differentiation ofagonist and antagonist activity in theGlycineB–iGluR–NMDA receptor, 2960

AIDS – Synthesis and anti–HIV activity eval-uation of2–(4–(naphthalen–2–yl)–1,2,3–thiadia-zol–5–ylthio)–N–acetamides as novelnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 4648

Air oxidation – SAR study of clubbed[1,2,4]–triazolyl with fluorobenzimidazolesas antimicrobial and antituberculosisagents, 2930

AKR1C1 inhibitors – New cyclopentanederivatives as inhibitors of steroid metabo-lizing enzymes AKR1C1 and AKR1C3,2563

AKR1C3 inhibitors – New cyclopentanederivatives as inhibitors of steroid metabo-lizing enzymes AKR1C1 and AKR1C3,2563

Akt/protein kinase B (PKB) inhibitors –QSAR study of Akt/protein kinase B (PKB)inhibitors using support vector machine,4090

Alamar blue assay – Synthesis and evaluationof in vitro anti–tuberculosis activity ofN–substituted glycolamides, 289

Albumin – Didanosine ester prodrugs:Synthesis, albumin binding properties andpharmacokinetic studies in rats, 3874

Aldehydes – Novel pyridazine derivatives:Synthesis and antimicrobial activity evalua-tion, 1989

ALK5 inhibitors – Synthesis and biologicalevaluation of benzenesulfonamide–substi-tuted 4–(6–alkylpyridin–2–yl)–5–(quinox-alin–6–yl)imidazoles as transforminggrowth factor–� type 1 receptor kinaseinhibitors, 568

Alkaloids – Aziridine alkaloids as potentialtherapeutic agents, 3373

Alkenyldiarylmethanes (ADAMs) –Synthesis of alkenyldiarylmethanes(ADAMs) containing benzo[d]isoxazoleand oxazolidin–2–one rings, a new series ofpotent non–nucleoside HIV–1 reverse tran-scriptase inhibitors, 1210

Alkylating agents – Sulphonamide–basedbombesin prodrug analogues for glutathione

Page 7: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5137

transferase, useful in targeted cancerchemotherapy, 2009

Alkylation – Acyclic nucleoside bisphospho-nates: Synthesis and properties of chiral2–amino–4,6–bis[(phosphonomethoxy)alkoxy]pyrimidines, 2408 – Synthesis and bio-logical evaluation of 3,6–disubstituted[1,2,4]triazolo[3,4–b][1,3,4]thiadiazolederivatives as a novel class of potentialanti–tumor agents, 2776 – SAR study ofclubbed [1,2,4]–triazolyl with fluorobenz-imidazoles as antimicrobial and antituber-culosis agents, 2930 – Synthesis, character-ization and evaluation of antibacterial activ-ity of some thiazolo[3,2–b][1,2,4]triazoleincorporating diphenylsulfone moieties,4752

Alkylene aminoguanidine derivatives –Synthesis and bioactivity of substitutedindan–1–ylideneaminoguanidine deriva-tives, 3771

Alkylidenethiosemicarbazide compounds –A class of potent tyrosinase inhibitors:Alkylidenethiosemicarbazide compounds,1773

Alkylphosphocholines – Dialkylamino andnitrogen heterocyclic analogues of hexade-cylphosphocholine and cetyltrimetylammo-nium bromide: Effect of phosphate groupand environment of the ammonium cationon their biological activity, 4970

Alkynes – Diamine–based human histamineH3 receptor antagonists:(4–Aminobutyn–1–yl)benzylamines, 4098

Allicin – Novel derivatives of 6–mercaptop-urine: Synthesis, characterization andantiproliferative activities ofS–allylthio–mercaptopurines, 541

All–trans–retinoic acid – Preparation of sper-mine conjugates with acidic retinoids withpotent ribonuclease P inhibitory activity, 2689

ALMOND – GRIND–based 3D–QSAR andCoMFA to investigate topics dominated byhydrophobic interactions: The case ofhERG K� channel blockers, 1926

Alzheimer disease – Perspectives in design-ing anti aggregation agents as Alzheimerdisease drugs, 3866

Alzheimer’s disease – Synthesis and activityof fibrillogenesis peptide inhibitors relatedto the 17–21 �–amyloid sequence, 179 –Design, synthesis, and evaluation of ben-zophenone derivatives as novel acetyl-cholinesterase inhibitors, 1341 –11C–labelled PIB analogues as potentialtracer agents for in vivo imaging of amyloid� in Alzheimer’s disease, 1415 – Synthesisand pharmacological evaluation of novelN–alkyl/aryl substituted thiazolidinonearecoline analogues as muscarinic receptor1 agonist in Alzheimer’s dementia models,4848

Alzheimer’s diseases – Active site directeddocking studies: Synthesis and pharmaco-logical evaluation of cis–2,6–dimethylpiperidine sulfonamides as inhibitors ofacetylcholinesterase, 4057

Amantadine – Polycyclic cage structures ascarrier molecules for neuroprotectivenon–steroidal anti–inflammatory drugs,2577

Amaryllidaceae – Anti–genotoxic hydrazidefrom Crinum defixum, 2754

Amastigote – Synthesis, biological evaluationand SAR of sulfonamide 4–methoxychal-cone derivatives with potential antileishma-nial activity, 755

AMD 3100 analogs – Bis–14–membered ringdiketal diamines: Synthesis and evaluationof their anti–HIV and anti–tumoral activi-ties, 3138

Amide group – 2–Azetidinone derivatives:Design, synthesis and evaluation of choles-terol absorption inhibitors, 1638

Amide – Synthesis of amidine and amide deriv-atives and their evaluation for anti–inflam-matory and analgesic activities, 1010

Amide–based ligands – Synthesis, structureand biological activity of copper(II) com-plexes of4–(2–pyridylmethyl)–1,7–dimethyl–1,4,7–triazonane–2,6–dione and4–(2–pyridylethyl)–1,7–dimethyl–1,4,7–tri-azonane–2,6–dione, 1607

Amidine – Synthesis of amidine and amidederivatives and their evaluation foranti–inflammatory and analgesic activities,1010

Amidrazones – Stereoselective synthesis andantimicrobial activity of benzofuran–based(1E)–1–(piperidin–1–yl)–N2–arylamidra-zones, 4985

Amination – Synthesis and biological evalua-tion of 3,6–disubstituted [1,2,4]triazo-lo[3,4–b][1,3,4]thiadiazole derivatives as anovel class of potential anti–tumor agents,2776

Amines – Amines and oximes derived fromdeoxybenzoins as Helicobacter pylori ure-ase inhibitors, 2246

Amino acid conjugates – Synthesis,anti–tuberculosis activity and 3D–QSARstudy of amino acid conjugates of4–(adamantan–1–yl) group containingquinolines, 2017

Amino acid – Discovering novelquercetin–3–O–amino acid–esters as a newclass of Src tyrosine kinase inhibitors, 1982– Effect of conjugates of all–trans–retinoicacid and shorter polyene chain analogueswith amino acids on prostate cancer cellgrowth, 3175

Amino acids – Synthesis, kinetic studies andpharmacological evaluation of mutual azoprodrugs of 5–aminosalicylic acid forcolon–specific drug delivery in inflammato-ry bowel disease, 3922

Amino imidazoles – Development of CoMFAand CoMSIA models of cytotoxicity data ofanti–HIV–1–phenylamino–1H–imidazolederivatives, 2400

Aminoacyl – Towards an efficient prodrug ofthe alkylating metabolite monomethyltri-azene: Synthesis and stability of N–acy-lamino acid derivatives of triazenes, 1049

Aminoacyl–tRNA synthetase –2–[2–Substituted–3–(3,4–dichlorobenzy-lamino)propylamino]–1H–quinolin–4–onesas Staphylococcus aureus methionyl–tRNAsynthetase inhibitors, 239

Aminoiminoisoxazoles – Synthesis, antimi-crobial and antioxidant activities of substi-

tuted pyrazoles, isoxazoles, pyrimidine andthioxopyrimidine derivatives, 4557

Aminomercaptotriazoles – Synthesis of3 , 6 – d i s u b s t i t u t e d7H–1,2,4–triazolo[3,4–b]–1,3,4–thiadi-azines as novel analgesic/anti–inflammato-ry compounds, 4528

Aminonitroimidazole – Synthesis of someN–substituted nitroimidazole derivatives aspotential antioxidant and antifungal agents,645

Amino–pyrimidine – A novel and efficientone step synthesis of 2–amino–5–cyano–6–hydroxy–4–aryl pyrimidines and theiranti–bacterial activity, 2651

Aminopeptidase N – Novel cyclic–imidepeptidomimetics as aminopeptidase Ninhibitors. Design, chemistry and activityevaluation. Part I, 4819

Aminophosphonates – Design, cytotoxic andfluorescent properties of novel N–phospho-rylalkyl substituted E,E–3,5–bis(aryli-dene)piperid–4–ones, 2135

Aminophosphonic acids – Synthesis, NMRcharacterization and in vitro antitumor eval-uation of new aminophosphonic aciddiesters, 3363

Aminophylline – A novel spectrophotometricmethod for the determination of amino-phylline with boric acid in pharmaceuticaland mixed serum samples, 1452

Aminoquinoline hybrid molecules – Recentdevelopments in the design and synthesis ofhybrid molecules basedon aminoquinolinering and their antiplasmodial evaluation, 3091

Ammine/ethylamine platinum(II) complex-es – Synthesis, characterization and cyto-toxicity of ammine/ethylamine platinum(II)complexes with carboxylates, 2758

Amodiaquine analogues – A new series ofamodiaquine analogues modified in thebasic side chain with in vitro antileishma-nial and antiplasmodial activity, 5071

Amoxicillin – Synthesis and biological evalu-ation of some thiazolidinone derivatives ofsteroid as antibacterial agents, 2597

Amyloid beta – Perspectives in designing antiaggregation agents as Alzheimer diseasedrugs, 3866

Amyloid – 11C–labelled PIB analogues aspotential tracer agents for in vivo imagingof amyloid � in Alzheimer’s disease, 1415

Amyrin ester derivatives – Synthesis of�–amyrin derivatives and their in vivo anti-hyperglycemic activity, 1215

A–5021 – Synthesis and anti–VZV activity of6–heteroaryl derivatives of tricyclic acy-clovir and 9–{[cis–1',2'–bis(hydrox-ymethyl)cycloprop–1'–yl]methyl}guanineanalogues, 3313

Anabolic activity – Synthesis andanabolic/androgenic evaluation of novel9�–fluorosteroids, 4567

Anacardic acid – Synthesis of benzamidederivatives of anacardic acid and their cyto-toxic activity, 2711

B��–Adrenoceptors blocking activity – Design,

synthesis and pharmacological evalua-

Page 8: Chal Micro

5138 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

tion of new 1–[3–(4–arylpiperazin–1–yl)–2–hydroxy–propyl]–3,3–diphenylpyrro-lidin–2–one derivatives with antiarrhyth-mic, antihypertensive, and ��–adrenolyticactivity, 3994

AAnalgesic activities – Design and synthesis of

azolopyrimidoquinolines, pyrimidoquina-zolines as anti–oxidant, anti–inflammatoryand analgesic activities, 609

Analgesic activity – Rare dipeptide and ureaderivatives from roots of Moringa oleiferaas potential anti–inflammatory andantinociceptive agents, 432 – Synthesis,analgesic and anti–inflammatory activitiesof novel 3–(4–acetamido–benzyl)–5–substi-tuted–1,2,4–oxadiazoles, 794 – Synthesisand pharmacological investigation of3–(substituted 1–phenylethanone)–4–(sub-stituted phenyl)–1, 2, 3, 4–tetrahydropyrim-idine–5–carboxylates, 3645

Analgesic agents – Regioselective reaction:Synthesis and pharmacological study ofMannich bases containing ibuprofen moi-ety, 3697

Analgesic – Conformationally constrained ana-logues of N'–(4–tert–butylbenzyl)–N–(4–methylsulfonylaminobenzyl)thiourea asTRPV1 antagonists, 322 – Synthesis andspectral characterization of a new class ofN–(N–methylpiperazinoacetyl)–2,6–diarylpiperidin–4–ones: Antimicrobial, analgesic andantipyretic studies, 577 – Synthesis of ami-dine and amide derivatives and their evalua-tion for anti–inflammatory and analgesicactivities, 1010 – New acyclic nucleosidesanalogues as potential analgesic, anti–inflam-matory, anti–oxidant and anti–microbialderived from pyrimido[4,5–b]quinolines,1427 – Synthesis and pharmacological evalu-ation of a novel series of5–(substituted)aryl–3–(3–coumarinyl)–1–phenyl–2–pyrazolines as novel anti–inflamma-tory and analgesic agents, 1682 – Synthesis,pharmacological screening, quantum chemi-cal and in vitro permeability studies ofN–Mannich bases of benzimidazoles throughbovine cornea, 2307 – Synthesis and pharma-cological evaluation of 2(3H)–furanones and2(3H)–pyrrolones, combining analgesic andanti–inflammatory properties with reducedgastrointestinal toxicity and lipid peroxida-tion, 2636 – Synthesis and pharmacologicalevaluation of N–phenyl–acetamide sulfon-amides designed as novel non–hepatotoxicanalgesic candidates, 3612 – Synthesis andanalgesic and anti–inflammatory activities6–substituted–3(2H)–pyridazinone–2–acetyl– 2 – ( p – s u b s t i t u t e d / n o n s u b s t i t u t e dbenzal)hydrazone derivatives, 3760 –Fenbufen based 3–[5–(substitutedaryl)–1,3,4–oxadiazol–2–yl]–1–(biphenyl–4–yl)propan–1–ones as safer antiinflammatoryand analgesic agents, 3798 – Synthesis andpharmacological evaluation of 1,3,4–oxadia-zole bearing bis(heterocycle) derivatives asanti–inflammatory and analgesic agents,3898 – S– and C–nucleosidoquinazoline asnew nucleoside analogs with potential anal-gesic and anti–inflammatory activity, 4249 –

Design, synthesis and pharmacologicalscreening of novel nitric oxide donors con-taining 1,5–diarylpyrazolin–3–one as nontox-ic NSAIDs, 4622 – Synthesis of6–aminomethyl derivatives of benzopy-ran–4–one with dual biological properties:Anti–inflammatory–analgesic and antimicro-bial, 4896

Analgesic/anti–inflammatory activity –Synthesis of 3,6–disubstituted7H–1,2,4–triazolo[3,4–b]–1,3,4–thiadi-azines as novel analgesic/anti–inflammato-ry compounds, 4528

B��–Alkylphenethylamine – Synthesis and

serotonin transporter activity of sul-phur–substituted ��–alkyl phenethy-lamines as a new class of anticancer agents,4862

AAnalogs of triclosan – Design and in silico

screening of combinatorial library of anti-malarial analogs of triclosan inhibitingPlasmodium falciparum enoyl–acyl carrierprotein reductase, 3009

B��–Aminophosphonates – Design and one–pot

synthesis of ��–aminophosphonates andbis(�–aminophosphonates) by iron(III)chloride and cytotoxic activity, 4266

��–Amyrin acetate – Synthesis of ��–amyrinderivatives and their in vivo antihyper-glycemic activity, 1215

AAnandamide – Synthesis and pharmacologi-

cal evaluation of sulfamide–based ana-logues of anandamide, 4889

Androgen – Steroidal lactones as inhibitors of17�–hydroxysteroid dehydrogenase type 5:Chemical synthesis, enzyme inhibitoryactivity, and assessment of estrogenic andandrogenic activities, 632

Androgenic activity – Synthesis and anabol-ic/androgenic evaluation of novel 9�–fluo-rosteroids, 4567

Androgens – Novel CYP17 inhibitors:Synthesis, biological evaluation,structure–activity relationships and model-ling of methoxy– and hydroxy–substitutedmethyleneimidazolyl biphenyls, 2765

Andrographolide – Synthesis and evaluationof antibacterial activities of andro-grapholide analogues, 2936

Androstane derivates – Synthesis and ana-bolic/androgenic evaluation of novel9�–fluorosteroids, 4567

Angiogenesis – Synthesis and biochemicalevaluation of a cyclic RGD oxorheniumcomplex as new ligand of �V�3 integrin,3394

B��–Halo compound – Synthesis and antibac-

terial activity of some new thiazole andthiophene derivatives, 4434

AAnhydrides – Synthesis and antitumor activi-

ty of some new xanthotoxin derivatives,2967

ANN – Comparative chemometric modelingof cytochrome 3A4 inhibitory activity ofstructurally diverse compounds using step-wise MLR, FA–MLR, PLS, GFA, G/PLSand ANN techniques, 2913

B��–Phthalimide ketones – The preparation and

in vitro antiproliferative activity of phthal-imide based ketones on MDAMB–231 andSKHep–1 human carcinoma cell lines,2736

��–Santonin derivatives – Synthesis and cyto-toxic activity of ��–santonin derivatives,3739

AA–seco triterpene – Synthesis and evaluation

of A–seco type triterpenoids foranti–HIV–1protease activity, 4112

Antagonist – Molecular orbital differentiationof agonist and antagonist activity in theGlycineB–iGluR–NMDA receptor, 2960

Anthracenyl phenylalanines – Synthesis ofnovel N–protected hydrophobic phenylala-nines and their application in potentialantibacterials, 1001

Anthrax – Modeling the activity of furininhibitors using artificial neural network,1664

Anti aggregation agents – Perspectives indesigning anti aggregation agents asAlzheimer disease drugs, 3866

Antiamoebic activity – Bis–pyrazolines:Synthesis, characterization and antiamoebicactivity as inhibitors of growth ofEntamoeba histolytica, 426 – New deriva-tives of 3,5–substituted–1,4,2–dioxazoles:Synthesis and activity against Entamoebahistolytica, 926

Antiarrhythmic – Synthesis, antiarrhythmicand anticoagulant activities of novel thiazo-lo derivatives from methyl2–(thiazol–2–ylcarbamoyl)acetate, 725 –Design, synthesis and pharmacologicalevaluation of new 1–[3–(4–arylpiper-azin–1–yl)–2–hydroxy–propyl]–3,3–diphenylpyrrolidin–2–one derivatives with antiar-rhythmic, antihypertensive, and�–adrenolytic activity, 3994

Antiarrhythmic, hypotensive and spas-molytic activities – Synthesis andadrenolytic activity of1–(1H–indol–4–yloxy)–3–{[2–(2–methoxyphenoxy)ethyl]amino}propan–2–ol and itsenantiomers. Part 1, 809

Antibacterial activity – Tetrahydronaphthylazole oxime ethers: The conformationallyrigid analogues of oxiconazole as antibacte-rials, 437 – Synthesis, biological evaluationand 2D–QSAR analysis of benzoxazoles asantimicrobial agents, 501 – Hansch analysisof veratric acid derivatives as antimicrobialagents, 689 – Synthesis and antibacterialactivity of nitroaryl thiadiazole–gatifloxacinhybrids, 1205 – A facile synthesis of novel

Page 9: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5139

biologically active 4–hydroxy–N'–(benzyli-dene)–2H–benzo[e][1,2]thiazine–3–carbo-hydrazide 1,1–dioxides, 1311 – Synthesis ofnew 2–substituted pyrido[2,3–d]pyrim-idin–4(1H)–ones and their antibacterialactivity, 1369 – Synthesis, structure andbiological activity of copper(II) complexeso f4–(2–pyridylmethyl)–1,7–dimethyl–1,4,7–triazonane–2,6–dione and4–(2–pyridylethyl)–1,7–dimethyl–1,4,7–tri-azonane–2,6–dione, 1607 – Synthesis andspectroscopic studies of biologically activecompounds derived from oxalyldihydrazideand benzil, and their Cr(III), Fe(III) andMn(III) complexes, 1731 – Synthesis andantibacterial evaluation of novel 4–alkylsubstituted phenyl �–aldehyde ketonederivatives, 1737 – Convenient one–potsynthesis of novel 2–substituted benzimida-zoles, tetrahydrobenzimidazoles and imida-zoles and evaluation of their in vitro anti-bacterial and antifungal activities, 1751 –Synthesis and antibacterial activity of somenew 2,3–dimethoxy–3–hydroxy–2–(1–phenyl–3–aryl–4–pyrazolyl)chro-manones, 1763 – Hansch analysis of substi-tuted benzoic acid benzylidene/furan–2–yl–methylene hydrazides asantimicrobial agents, 1853 – DNA bindingand antimicrobial studies of polymer–cop-per(II) complexes containing 1,10–phenan-throline and l–phenylalanine ligands, 1878– Design, synthesis and antibacterial activi-ty of novel actinonin derivatives containingbenzimidazole heterocycles, 2202 –Examination of growth inhibitory propertiesof synthetic chalcones for which antibacter-ial activity was predicted, 2211 –Organoiodine (III)–mediated synthesis of3–aryl/heteroaryl–5,7–dimethyl–1,2,4–tria-zolo[4,3–c]pyrimidines as antibacterialagents, 2260 – Synthesis, spectral studiesand in vitro antibacterial activity ofsteroidal thiosemicarbazone and their palla-dium (Pd (II)) complexes, 2270 – Synthesisand evaluation of some new benzimidazolederivatives as potential antimicrobialagents, 2294 – Synthesis, antimicrobial andantiviral evaluation of substituted imidazolederivatives, 2347 – Synthesis and biologicalevaluation of some thiazolidinone deriva-tives of steroid as antibacterial agents, 2597– Synthesis and antimicrobial studies ofnovel methylene bridged benzisoxazolylimidazo[2,1–b][1,3,4]thiadiazole deriva-tives, 2828 – SAR study of clubbed[1,2,4]–triazolyl with fluorobenzimidazolesas antimicrobial and antituberculosisagents, 2930 – Synthesis of novel carbazolebased macrocyclic amides as potentialantimicrobial agents, 3040 – Synthesis,characterization and antibacterial activity ofsome triazole Mannich bases carryingdiphenylsulfone moieties, 3083 –Mechanism of unusual formation of3–(5–phenyl–3H–[1,2,4]dithiazol–3–yl)chromen–4–ones and4–oxo–4H–chromene–3–carbothioic acidN–phenylamides and their antimicrobialevaluation, 3209 – Copper(II) and uranyl(II)

complexes with acylthiosemicarbazide:Synthesis, characterization, antibacterialactivity and effects on the growth ofpromyelocytic leukemia cells HL–60, 3323– Mono andbis–6–arylbenzimidazo[1,2–c]quinazolines:A new class of antimicrobial agents, 3330 –Novel ureas and thioureas of 15–memberedazalides with antibacterial activity againstkey respiratory pathogens, 3459 –Regioselective reaction: Synthesis, charac-terization and pharmacological studies ofsome new Mannich bases derived from1,2,4–triazoles, 3784 – A facile one–potgreen synthesis and antibacterial activity of2–amino–4H–pyrans and2–amino–5–oxo–5,6,7,8–tetrahydro–4H–chromenes, 3805 – Synthesis, structure andstructure–activity relationship analysis of3–tert–butoxycarbonyl–2–arylthiazoli-dine–4–carboxylic acid derivatives aspotential antibacterial agents, 3903 –Synthesis and antibacterial activity of novel15–membered macrolide derivatives:4"–Carbamate, 11,12–cyclic carbon-ate–4"–carbamate and 11,4"–di–O–arylcar-bamoyl analogs of azithromycin, 4010 –Synthesis and in vitro antibacterial activityof 7–(4–alkoxyimino–3–amino–3–methylpiperidin–1–yl)fluoroquinolonederivatives, 4063 – Inhibitory effects of5–benzylidene barbiturate derivatives onmushroom tyrosinase and their antibacterialactivities, 4235 – Synthesis, crystal struc-tures and antibacterial activity studies ofaza–derivatives of phytoalexin from cottonplant – gossypol, 4393 – Synthesis and anti-bacterial activity of some new thiazole andthiophene derivatives, 4434 – Synthesis,spectroscopic characterization and antibac-terial activity of new cobalt(II) complexesof unsymmetrical tetradentate (OSN2)Schiff base ligands, 4490 – Synthesis, char-acterization and antibacterial activity of2–[1–(5–chloro–2–methoxy–phenyl)–5–methyl–1H–pyrazol–4–yl]–5–(substituted–phenyl)–[1,3,4]oxadiazoles, 4522 – Synthesisand antimicrobial activities of novel quino-line derivatives carrying 1,2,4–triazole moi-ety, 4637 – Synthesis, photochemical E(trans)�Z (cis) isomerization and antimi-crobial activity of 2–chloro–5–methylpyri-dine–3–olefin derivatives, 4661 – Design,synthesis and in vitro antibacterial/antifun-gal evaluation of novel1–ethyl–6–fluo-ro–1,4–dihydro–4–oxo–7(1–piperazinyl)quinoline–3–carboxylicacid derivatives, 4726– Synthesis, characterization and evaluationof antibacterial activity of some thiazo-lo[3,2–b][1,2,4]triazole incorporatingdiphenylsulfone moieties, 4752 – Synthesisand antibacterial activity of some novelbis–1,2,4–triazolo[3,4–b]–1,3,4–thiadia-zoles and bis–4–thiazolidinone derivativesfrom terephthalic dihydrazide, 5112

Antibacterial agents – Synthesis and biologi-cal evaluation of novel luteolin derivativesas antibacterial agents, 908 – Synthesis andantibacterial activity of some new thiadi-a z a / t r i a z a p h o s p h o l e s ,thiadiaza/triaza/tetrazaphosphinines and

thiadiaza/tetrazaphosphepines containing1,2,4–triazinone moiety, 4539

Antibacterial and antifungal activities –Some O,O',O",O–di/tetra aryldithioimi-dophonate transition metal complexesderived from catechol and bisphenol–A asantibacterial and antifungal agents, 785

Antibacterial drugs – Multi–target spectralmoments for QSAR and Complex Networksstudy of antibacterial drugs, 4516

Antibacterial – Synthesis and QSAR model-ing of 2–acetyl–2–ethoxycar-bonyl–1–[4(4'–arylazo)–phenyl]–N,N–dimethylaminophenyl aziridines as potentialantibacterial agents, 251 – Synthesis, opti-mization and structure–activity relation-ships of 3,5–disubstituted isoxazolines asnew anti–tuberculosis agents, 460 –Synthesis and antimicrobial activities ofsome new triazolothiadiazoles bearing4–methylthiobenzyl moiety, 551 –Synthesis of novel benzo[h]quinolines:Wound healing, antibacterial, DNA bindingand in vitro antioxidant activity, 981 –Synthesis and in vitro antimicrobial activityof some novel substituted benzimidazolederivatives having potent activity againstMRSA, 1024 – Synthesis, characterizationand antimicrobial activity of water solubledendritic macromolecules, 1093 –Antimicrobial studies of some novel quina-zolinones fused with [1,2,4]–triazole,[1,2,4]–triazine and [1,2,4,5]–tetrazinerings, 1188 – Synthesis, characterizationand structure–activity relationship analysisof novel depsides as potential antibacterials,1779 – Fullerene derivatized s–triazine ana-logues as antimicrobial agents, 2178 –Design, synthesis and biological evaluationof novel nitrogen and sulfur containing het-ero–1,4–naphthoquinones as potent antifun-gal and antibacterial agents, 3130 –Synthesis and antibacterial activity of novel5–(4–methyl–1H–1,2,3–triazole) methyloxazolidinones, 3217 – Aziridine alkaloidsas potential therapeutic agents, 3373 –Antioxidant and antibacterial studies of ary-lazopyrazoles and arylhydrazonopyra-zolones containing coumarin moiety, 4690 –Synthesis of new 4–isopropylthiazolehydrazide analogs and some derivedclubbed triazole, oxadiazole ring systems –A novel class of potential antibacterial, anti-fungal and antitubercular agents, 4739

Antibacterial screening – Phase transfer cat-alyzed synthesis of bis–quinolines:Antileishmanial activity in experimentalvisceral leishmaniasis and in vitro antibac-terial evaluation, 845

Antibacterials – Synthesis of novel N–pro-tected hydrophobic phenylalanines andtheir application in potential antibacterials,1001

Antibiotic – 2–[2–Substituted–3–(3,4–dichlorobenzylamino)propylamino]–1H–quinolin–4–ones as Staphylococcus aureusmethionyl–tRNA synthetase inhibitors, 239

Antibody – Potential of mean force forSyrian hamster prion epitope protein –Monoclonal fab 3f4 antibody interactionstudies, 3504

Page 10: Chal Micro

5140 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Anticancer activity – Possible anticanceragents: QSAR analogs of glutamamide:Synthesis and pharmacological activity of1,5–N,N'–disubstituted–2–(substituted ben-zenesulphonyl) glutamamides, 70 –Synthesis of novel thiazolone–based com-pounds containing pyrazoline moiety andevaluation of their anticancer activity, 1396– Synthesis, structure and biological activi-ty of copper(II) complexes of 4–(2–pyridyl-methyl)–1,7–dimethyl–1,4,7–triazo-nane–2,6–dione and4–(2–pyridylethyl)–1,7–dimethyl–1,4,7–tri-azonane–2,6–dione, 1607 – CoMFA anddocking studies of 2–phenylindole deriva-tives with anticancer activity, 2822 – Totalsynthesis and anticancer activity of highlypotent novel glycolipid derivatives, 3120 –Synthesis, antiviral and anticancer activityof some novel thioureas derivedfromN–(4–nitro–2–phenoxyphenyl)–methane-sulfonamide, 3591 – Synthesis and in vitroanticancer activity of2,4–azolidinedione–acetic acids derivatives,3627 – Synthesis, structure elucidation andantitumour activity of N–substituted amideso f3–(3–ethylthio–1,2,4–triazol–5–yl)propenoic acid, 3788 – In vitro and in vivo anti-cancer activity of 2–deacetoxytaxinine Jand synthesis of novel taxoids and their invitro anticancer activity, 3947 – NovelBiginelli dihydropyrimidines with potentialanticancer activity: A parallel synthesis andCoMSIA study, 4192 – Synthesis and anti-cancer activity ofN–bis(trifluoromethyl)alkyl–N'–thiazolyland N–bis(trifluoromethyl)alkyl–N'–ben-zothiazolyl ureas, 4944 – Synthesis andantitumor activity studies of some newfused 1,2,4–triazole derivatives carrying2,4–dichloro–5–fluorophenyl moiety, 5066

Anticancer agents – New cyclopentane deriv-atives as inhibitors of steroid metabolizingenzymes AKR1C1 and AKR1C3, 2563 –Design, synthesis and preliminary biologi-cal evaluation of N–hydroxy–4–(3–phenyl-propanamido)benzamide (HPPB) deriva-tives as novel histone deacetylase inhibitors,4470

Anticancer drugs – Scoring function forDNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Anticancer – Synthesis and biological evalu-ation of novel symmetry bis–enediynes, 35– Aziridine alkaloids as potential therapeu-tic agents, 3373 – Design, synthesis andanticancer evaluation of novel tetrahydro-quinoline derivatives containing sulfon-amide moiety, 4211

Anticancer therapy – Metals in anticancertherapy: Copper(II) complexes as inhibitorsof the 20S proteasome, 4353

Antichagasic in vivo activity –5–Nitro–2–furyl derivative actives againstTrypanosoma cruzi: Preliminary in vivostudies, 3909

Anticoagulant activities – Synthesis, antiar-rhythmic and anticoagulant activities of

novel thiazolo derivatives from methyl2–(thiazol–2–ylcarbamoyl)acetate, 725

Anticoagulant – Design of novel aminopyrro-lidine factor Xa inhibitors from a screeninghit, 2787

Anticoagulants – On designing non–saccha-ride, allosteric activators of antithrombin,2626

Anticoccidial drug – Predicting the activityof drugs for a group of imidazopyridineanticoccidial compounds, 4044

Anticonvulsant activity – Synthesis of somen o v e lN4–(naphtha[1,2–d]thiazol–2–yl)semicar-bazides as potential anticonvulsants, 203 –Synthesis and potential anticonvulsantactivity of new N–3–substituted 5,5–cyclo-propanespirohydantoins, 296 – Synthesisand anticonvulsant activity of some substi-tuted 1,2,4–thiadiazoles, 1100 – Synthesisof some new4–styryltetrazolo[1,5–a]quinoxaline and1–substituted–4–styryl[1,2,4]triazolo[4,3–a]quinoxaline derivatives as potent anticon-vulsants, 1135 – Synthesis and anticonvul-sant activity of new N–[(4–arylpiper-azin–1–yl)–alkyl] derivatives of3–phenyl–pyrrolidine–2,5–dione, 2224

Anticonvulsant – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Synthesis, antibacterial and anticonvul-sant evaluations of some cyclic enaminones,967 – Design, synthesis of8–alkoxy–5,6–dihydro–[1,2,4]triazino[4,3–a]quinolin–1–ones with anticonvulsantactivity, 1265 – Solution–phase parallelsynthesis and evaluation of anticonvulsantactivity of N–substituted–3,4–dihydroiso-quinoline–2(1H)–carboxamides, 1349 –Synthesis of novel pyrazole derivatives andevaluation of their antidepressant and anti-convulsant activities, 3480

Anticonvulsants – Synthesis and anticonvul-sant activity of some new bishydrazonesderived from 3,4–dipropyloxythiophene,3672 – A new class of anticonvulsants pos-sessing 6Hz activity: 3,4–Dialkyloxy thio-phene bishydrazones, 4376

Antidepressant activities – Quantitativestructure–activity relationship analysis ofaryl alkanol piperazine derivatives withantidepressant activities, 4367

Antidepressant activity – Synthesis and sero-tonin receptor activity of the arylpiperazinealkyl/propoxy derivatives of new azatricy-cloundecanes, 152

Antidepressant drugs – Molecular propertiesof psychopharmacological drugs determin-ing non–competitive inhibition of 5–HT3Areceptors, 2667

Antidepressant – Synthesis of novel pyrazolederivatives and evaluation of their antide-pressant and anticonvulsant activities, 3480

Antidepressants – Novel4–aryl–pyrido[1,2–c]pyrimidines with dualSSRI and 5–HT1A activity, Part 1, 1710 –Novel 4–aryl–pyrido[1,2–c]pyrimidines withdual SSRI and 5–HT1A activity: Part 2, 4702

Antidiabetic activity – Novel 2–aryl–naph-tho[1,2–d]oxazole derivatives as potential

PTP–1B inhibitors showing antihyper-glycemic activities, 109

Antidiabetic effects on pancreas – Synthesis,characterization and antidiabetic propertieso fN1–2,4–dihydroxybenzylidene–N4–2–hydroxybenzylidene–S–methyl–thiosemicar-bazidato–oxovanadium(IV), 818

Antidiabetic – Synthesis and in vivo antidia-betic activity of novel dispiropyrrolidinesthrough [3�2] cycloaddition reactions withthiazolidinedione and rhodanine deriva-tives, 3272

Antidiuretic activity – Arginine vasopressinand its analogues – The influence of posi-tion 2 modification with 3,3–diphenylala-nine enantiomers. Highly potent V2 ago-nists, 2862

Antifungal activity – Synthesis, biologicalevaluation and 2D–QSAR analysis of ben-zoxazoles as antimicrobial agents, 501 –Synthesis of some N–substituted nitroimi-dazole derivatives as potential antioxidantand antifungal agents, 645 – Hansch analy-sis of veratric acid derivatives as antimicro-bial agents, 689 – Antimicrobial studies ofsome novel quinazolinones fused with[1,2,4]–triazole, [1,2,4]–triazine and[1,2,4,5]–tetrazine rings, 1188 –2–Acylhydrazino–5–arylpyrrole deriva-tives: Synthesis and antifungal activity eval-uation, 1288 – Convenient one–pot synthe-sis of novel 2–substituted benzimidazoles,tetrahydrobenzimidazoles and imidazolesand evaluation of their in vitro antibacterialand antifungal activities, 1751 – Antifungalunsaturated cyclic Mannich ketones andamino alcohols: Study of mechanism ofaction, 1823 – Hansch analysis of substitut-ed benzoic acidbenzyl idene / furan–2–yl–methylenehydrazides as antimicrobial agents, 1853 –DNA binding and antimicrobial studies ofpolymer–copper(II) complexes containing1,10–phenanthroline and l–phenylalanineligands, 1878 – Design, synthesis, and bio-logical evaluation of novel triazole deriva-tives as inhibitors of cytochrome P45014�–demethylase, 1913 – Synthesis andevaluation of some new benzimidazolederivatives as potential antimicrobialagents, 2294 – Synthesis, antimicrobial andantiviral evaluation of substituted imidazolederivatives, 2347 – Synthesis, antifungalactivities and 3D–QSAR study ofN–(5–substituted–1,3,4–thiadiazol–2–yl)cyclopropanecarboxamides, 2782 – Synthesisand antimicrobial studies of novel methyl-ene bridged benzisoxazolylimidazo[2,1–b][1,3,4]thiadiazole deriva-tives, 2828 – Synthesis of novel carbazolebased macrocyclic amides as potentialantimicrobial agents, 3040 – Design, syn-thesis, and antifungal activity of triazole andbenzotriazole derivatives, 3064 –Mechanism of unusual formation of3–(5–phenyl–3H–[1,2,4]dithiazol–3–yl)chromen–4–ones and4–oxo–4H–chromene–3–carbothioic acidN–phenylamides and their antimicrobialevaluation, 3209 – Mono and bis–6–aryl-

Page 11: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5141

benzimidazo[1,2–c]quinazolines: A newclass of antimicrobial agents, 3330 –Regioselective reaction: Synthesis, charac-terization and pharmacological studies ofsome new Mannich bases derived from1,2,4–triazoles, 3784 – Synthesis, physico-chemical properties and antimicrobial activ-ity of some new benzimidazole derivatives,4028 – New azoles with potent antifungalactivity: Design, synthesis and moleculardocking, 4218 – Synthesis and antimicro-bial activities of novel quinoline derivativescarrying 1,2,4–triazole moiety, 4637 –Synthesis, photochemical E (trans)�Z (cis)isomerization and antimicrobial activity of2–chloro–5–methylpyridine–3–olefinderivatives, 4661 – Design, synthesis and invitro antibacterial/antifungal evaluation ofnovel1–ethyl–6–fluoro–1,4–dihydro–4–oxo–7(1–piperazinyl)quinoline–3–carboxyli-cacid derivatives, 4726 – Dialkylamino andnitrogen heterocyclic analogues of hexade-cylphosphocholine and cetyltrimetylammo-nium bromide: Effect of phosphate groupand environment of the ammonium cationon their biological activity, 4970

Antifungal agent – The structure–bioavail-ability approach in antifungal agents, 1978

Antifungal agents – A facile synthesis of�,�'–(EE)–bis(benzylidene)–cycloalka-nones and their antitubercular evaluations,1705 – Synthesis and antiparasitic and anti-fungal evaluation of 2'–arylsubstituted–1H,1'H–[2,5']bisbenzimidazolyl–5–carbox-amidines, 2002

Antifungal compounds – Scoring functionfor DNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Antifungal drugs – Multi–target spectralmoment: QSAR for antifungal drugs vs. dif-ferent fungi species, 4051

Antifungal – Synthesis and antimicrobialactivities of some new triazolothiadiazolesbearing 4–methylthiobenzyl moiety, 551 –Synthesis and in vitro antimicrobial activityof some novel substituted benzimidazolederivatives having potent activity againstMRSA, 1024 –2,3–Disubstituted–1,4–naphthoquinones,12H–benzo[b]phenothiazine–6,11–dionesand related compounds: Synthesis andBiological evaluation as potential antiprolif-erative and antifungal agents, 1086 –Photodynamic inactivation of Candida albi-cans sensitized by tri– and tetra–cationicporphyrin derivatives, 1592 – Design, syn-thesis and biological evaluation of novelnitrogen and sulfur containinghetero–1,4–naphthoquinones as potent anti-fungal and antibacterial agents, 3130 –Synthesis, characterization and derivatiza-tion of some novel types of mono– andbis–imidazolidineiminothiones and imida-zolidineiminodithiones with antitumor,antiviral, antibacterial and antifungal activi-ties – part I, 4315 – Synthesis of new 4–iso-propylthiazole hydrazide analogs and somederived clubbed triazole, oxadiazole ringsystems – A novel class of potential antibac-

terial, antifungal and antitubercular agents,4739

Antihyperglycemic activity – Synthesis of�–amyrin derivatives and their in vivo anti-hyperglycemic activity, 1215

Antihypertensive activity – Synthesis andpharmacological investigation of 3–(substi-tuted 1–phenylethanone)–4–(substitutedphenyl)–1, 2, 3, 4–tetrahydropyrimi-dine–5–carboxylates, 3645

Antiinflammatory – Fenbufen based3–[5–(substituted aryl)–1,3,4–oxadia-zol–2–yl]–1–(biphenyl–4–yl)propan–1–ones as safer antiinflammatory and analgesicagents, 3798

Antileishmanial activity – Phase transfer cat-alyzed synthesis of bis–quinolines:Antileishmanial activity in experimentalvisceral leishmaniasis and in vitro antibac-terial evaluation, 845

Antileishmanial – Synthesis and antiproto-zoal activities of dicationic bis(phe-noxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Antileukotrienic activity – Antileukotrienicphenethylamido derivatives of arylalkanoicacids in the treatment of ulcerative colitis,332

Antimalarial activity – Synthesis ofchlorovinyl sulfones as structural analogs ofchalcones and their antiplasmodial activi-ties, 1457 – Synthesis and antimalarialactivity of new atovaquone derivatives,4778

Antimalarial chalcone combination –Antimalarial pharmacodynamics of chal-cone derivatives in combination withartemisinin against Plasmodium falciparumin vitro, 3388

Antimalarial – Search for new pharma-cophores for antimalarial activity. Part III:Synthesis and bioevaluation of new6–thioureido–4–anilinoquinazolines, 4404

Antimicrobial activity – Synthesis of newseries of 5,6–dihydro–4H–1,2–oxazines viahetero Diels–Alder reaction and evaluationof antimicrobial activity, 280 – Synthesis ofsome new 1,2,4–triazoles, their Mannichand Schiff bases and evaluation of theirantimicrobial activities, 1057 – Synthesisand QSAR evaluation of 2–(substitutedphenyl)–1H–benzimidazoles and [2–(sub-stituted phenyl)–benzimidazol–1–yl]–pyridin–3–yl–methanones, 1119 –Synthesis, characterization and antimicro-bial activity of Co(II), Zn(II) and Cd(II)complexes with N–benzyloxycarbonyl–S–phenylalanine, 1537 – Novel pyridazinederivatives: Synthesis and antimicrobialactivity evaluation, 1989 – Synthesis,antimicrobial and cytotoxic activities ofsome 5–arylidene–4–thioxo–thiazoli-dine–2–ones, 2038 – Synthesis, antimicro-bial and cytotoxic activities of 1,3,4–oxadi-azoles, 1,3,4–thiadiazoles and 1,2,4–tria-zoles, 2106 – Synthesis, antimicrobial eval-uation and QSAR study of some 3–hydrox-ypyridine–4–one and 3–hydroxypyran–4–one derivatives, 2145 – Synthesis andantimicrobial activity of new 1–alkyl/cyclo-

hexyl–3,3–diaryl–1'–methylspiro[azeti-dine–2,3'–indoline]–2',4–diones, 2265 –Diazinium salts with dihydroxyacetophe-none skeleton: Syntheses and antimicrobialactivity, 2275 – Synthesis and bioassay of anew class of heterocycles pyrrolyl oxadia-zoles/thiadiazoles/triazoles, 2313 –Antimicrobial and SOD activities of noveltransition metal ternary complexes of imin-odiacetic acid containing �–diimine as aux-iliary ligand, 2517 – Physicochemical andbiological characterization of novel macro-cycles derived from o–phthalaldehyde,2621 – Synthesis and antimicrobial evalua-tion of 1–(benzofuran–2–yl)–4–nitro–3–arylbutan–1–ones and 3–(benzofu-ran–2–yl)–4,5–dihydro–5–aryl–1–[4–(aryl)–1,3–thiazol–2–yl]–1H–pyrazoles, 2632 –Hybrid molecules between benzenesulfon-amides and active antimicrobialbenzo[d]isothiazol–3–ones, 2741 –Synthesis of some new 1,3,4–thiadia-zol–2–ylmethyl–1,2,4–triazole derivativesand investigation of their antimicrobialactivities, 2896 – Copper complexes ofpyridine derivatives with superoxide scav-enging and antimicrobial activities, 3259 –Antimicrobial active macrocyclic complex-es of Cr(III), Mn(III) and Fe(III) with theirspectroscopic approach, 3299 – Convenientsynthesis and antimicrobial evaluation ofsome novel 2–substituted–3–methylbenzo-furan derivatives, 3637 – Synthesis, physic-ochemical properties and antimicrobialactivity of some new benzimidazole deriva-tives, 4028 – Synthesis, characterizationand in vitro antimicrobial activity of novel2–thioxo–4–thiazolidinones and4,4'–bis(2–thioxo–4–thiazolidinone–3–yl)diphenylsulfones, 4148 – Synthesis, spectraland biological evaluation of some new thia-zolidinones and thiazoles based ont–3–alkyl–r–2,c–6–diarylpiperidin–4–ones,4199 – Synthesis of some new 1,2,4–tria-zoles starting from isonicotinic acidhydrazide and evaluation of their antimicro-bial activities, 4362 – Synthesis of somenovel pyrazolo[3,4–b]pyridine and pyrazo-lo[3,4–d]pyrimidine derivatives bearing5,6–diphenyl–1,2,4–triazine moiety aspotential antimicrobial agents, 4385 –Synthesis, antimicrobial and antioxidantactivities of substituted pyrazoles, isoxa-zoles, pyrimidine and thioxopyrimidinederivatives, 4557 – Enaminonitrile in hete-rocyclic synthesis: Synthesis and antimicro-bial evaluation of some new pyrazole, isox-azole and pyrimidine derivatives incorpo-rating a benzothiazole moiety, 4813 –Stereoselective synthesis and antimicrobialactivity of benzofuran–based(1E)–1–(piperidin–1–yl)–N2–arylamidra-zones, 4985 – Synthesis and antimicrobialactivity of some new N–acyl substitutedphenothiazines, 5094

Antimicrobial agent – Synthesis and biologi-cal evaluation of a novel series of 1,5–ben-zothiazepine derivatives as potential antimi-crobial agents, 2815

Antimicrobial and antifungal activities –Application of phosphonyl carbanions to

Page 12: Chal Micro

5142 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

highly regioselective synthesis of somediazaphospholes and pyrazolinyl phospho-nates, 526

Antimicrobial – Synthesis and spectral char-acterization of a new class ofN–(N–methylpiperazinoacetyl)–2,6–diarylpiperidin–4–ones: Antimicrobial, analgesicand antipyretic studies, 577 – Synthesis,characterization, antimicrobial and antitu-mor screening of some diorganotin(IV)complexes of2–[(9H–Purin–6–ylimino)]–phenol, 3981 –Synthesis, characterization and derivatiza-tion of some novel types of mono– andbis–imidazolidineiminothiones and imida-zolidineiminodithiones with antitumor,antiviral, antibacterial and antifungal activi-ties – part I, 4315 – Synthesis of6–aminomethyl derivatives of benzopy-ran–4–one with dual biological properties:Anti–inflammatory–analgesic and antimi-crobial, 4896

Antimicrobial properties – Cationic surfac-tants from lysine: Synthesis, micellizationand biological evaluation, 1884 –Regioselective synthetic approachestowards 1,2,8,9–tetraazadispiro[4.1.4.2]trideca–2,9–dien–6–ones of potentialantimicrobial properties, 2447

Antimicrobials – Tetrahydronaphthyl azoleoxime ethers: The conformationally rigidanalogues of oxiconazole as antibacterials,437

Antimycobacterial activity – Preparation andin vitro evaluation of benzylsulfanyl ben-zoxazole derivatives as potential antituber-culosis agents, 2286 – A facile synthesis andantimycobacterial evaluation of novelspiro–pyrido–pyrrolizines and pyrrolidines,3821 – Design, synthesis and antimycobac-terial activity of some novelimidazo[1,2–c]pyrimidines, 3837 –Synthesis, spectral and biological evalua-tion of some new thiazolidinones and thia-zoles based ont–3–alkyl–r–2,c–6–diarylpiperidin–4–ones,4199 – Synthesis and antimycobacterialactivity of N'–[(E)–(monosubstituted–ben-zylidene)]–2–pyrazinecarbohydrazidederivatives, 4954 – l–Proline–catalysedfacile green protocol for the synthesis andantimycobacterial evaluation of [1,4]–thi-azines, 4978

Antimycobacterial – Synthesis and antimy-cobacterial activities of novel 6–nitro-quinolone–3–carboxylic acids, 345 –Diversity–oriented synthesis offuro[3,2–f]chromanes with antimycobacter-ial activity, 2497 – SAR study of clubbed[1,2,4]–triazolyl with fluorobenzimidazolesas antimicrobial and antituberculosisagents, 2930 – Novel4–(morpholin–4–yl)–N'–(arylidene)benzo-hydrazides: Synthesis, antimycobacterialactivity and QSAR investigations, 3954

Antimycotic activity – Synthesis and biologi-cal evaluation of abietic acid derivatives,2468

Anti–aggregant and pro–aggregant activi-ties – Circular dichroism studies of type IIIcollagen mimetic peptides with anti– or

pro–aggregant activities on human platelets,2643

Anti–bacterial activity – A novel and effi-cient one step synthesis of2–amino–5–cyano–6–hydroxy–4–arylpyrimidines and their anti–bacterial activity,2651

Anti–bacterial – Synthesis and anti–micro-bial screening of some Schiff bases of3–amino–6,8–dibromo–2–phenylquina-zolin–4(3H)–ones, 2328

Anti–diabetic activity – Synthesis and evalu-ation of some novel isochroman carboxylicacid derivatives as potential anti–diabeticagents, 3147

Anti–diabetic agent – Synthesis and evalua-tion of structurally constrained imidazolidinderivatives as potent dipeptidyl peptidaseIV inhibitors, 3318

Antineoplastic therapy –Sulphonamide–based bombesin prodruganalogues for glutathione transferase, usefulin targeted cancer chemotherapy, 2009

Anti–fungal – Synthesis and anti–microbialscreening of some Schiff bases of3–amino–6,8–dibromo–2–phenylquina-zolin–4(3H)–ones, 2328 – Anti–oxidant,anti–fungal and anti–leishmanial activitiesof novel3–[4–(1H–imidazol–1–yl)phenyl]prop–2–en–1–ones, 4654

Anti–genotoxicity – Anti–genotoxichydrazide from Crinum defixum, 2754

Anti–HIV activity – Synthesis and anti–HIVstudies of 2– and 3–adamantyl–substitutedthiazolidin–4–ones, 303

Anti–HIV – Synthesis, HIV–RT inhibitoryactivity and SAR of1–benzyl–1H–1,2,3–triazole derivatives ofcarbohydrates, 373 – Predicting anti–HIVactivity of 1,3,4–thiazolidinone derivatives:3D–QSAR approach, 1180 – Synthesis ofalkenyldiarylmethanes (ADAMs) contain-ing benzo[d]isoxazole andoxazolidin–2–one rings, a new series ofpotent non–nucleoside HIV–1 reverse tran-scriptase inhibitors, 1210 – Development ofCoMFA and CoMSIA models of cytotoxici-ty data ofanti–HIV–1–phenylamino–1H–imidazolederivatives, 2400

Anti–HIV–1 activity – Anti–HIV evaluationof benzo[d]isothiazole hydrazones, 1801

Anti–inflammation – Synthesis, crystal struc-ture and anti–inflammatory properties ofcurcumin analogues, 915

Anti–inflammatory activities – New acyclicnucleosides analogues as potential anal-gesic, anti–inflammatory, anti–oxidant andanti–microbial derived frompyrimido[4,5–b]quinolines, 1427

Anti–inflammatory activity – Synthesis andanti–inflammatory activity of newer quina-zolin–4–one derivatives, 83 – Synthesis,analgesic and anti–inflammatory activitiesof novel 3–(4–acetamido–benzyl)–5–substi-tuted–1,2,4–oxadiazoles, 794 – Synthesisand pharmacological investigation of3–(substituted 1–phenylethanone)–4–(sub-stituted phenyl)–1, 2, 3, 4–tetrahydropyrim-idine–5–carboxylates, 3645 – Synthesis andanalgesic and anti–inflammatory activities

6–substituted–3(2H)–pyridazinone–2–acetyl – 2 – ( p – s u b s t i t u t e d / n o n s u b s t i t u t e dbenzal)hydrazone derivatives, 3760 –Synthesis and anti–inflammatory evaluationof novel angularly or linearly fusedcoumarins, 5012

Anti–inflammatory agents and transcrip-tion inhibitors – Design, synthesis andcharacterization of novel 2–(2,4–disubsti-tuted–thiazole–5–yl)–3–aryl–3H–quinazo-line–4–one derivatives as inhibitors ofNF–�B and AP–1 mediated transcriptionactivation and as potential anti–inflammato-ry agents, 2184

Anti–inflammatory agents – Design and syn-thesis of new N–(fluorenyl–9–methoxycar-bonyl) (Fmoc)–dipeptides as anti–inflam-matory agents, 1933 – Aroylpropionic acidbased 2,5–disubstituted–1,3,4–oxadiazoles:Synthesis and their anti–inflammatory andanalgesic activities, 2372 – Regioselectivereaction: Synthesis and pharmacologicalstudy of Mannich bases containing ibupro-fen moiety, 3697

Anti–inflammatory and analgesic – Synthesisand pharmacological evaluation of 2–substi-tuted benzo[b]thiophenes as anti–inflamma-tory and analgesic agents, 1718 – Synthesis,analgesic and anti–inflammatory activitiesevaluation of some bi–, tri– and tetracycliccondensed pyrimidines, 4572

Anti–inflammatory drugs – Synthesis, phar-macological evaluation and docking studiesof new sulindac analogues, 1959

Anti–inflammatory – Regioselective synthe-sis of dispiro[1H–indene–2,3'–pyrroli-dine–2',3"–[3H]indole]–1,2"(1"H)–dionesof potential anti–tumor properties, 91 –Design, synthesis and molecular modelingstudy of acylated 1,2,4–triazole–3–acetateswith potential anti–inflammatory activity,117 – Design and synthesis of azolopyrimi-doquinolines, pyrimidoquinazolines asanti–oxidant, anti–inflammatory and anal-gesic activities, 609 – Synthesis of amidineand amide derivatives and their evaluationfor anti–inflammatory and analgesic activi-ties, 1010 – Adamantane derivatives of thi-azolyl–N–substituted amide, as possiblenon–steroidal anti–inflammatory agents,1198 – Regioselective synthesis and stereo-chemical structure of anti–tumor activedispiro[3H–indole–3,2'–pyrrolidine–3',3'–piperidine]–2(1H),4"–diones, 1257 –Synthesis and pharmacological evaluationof a novel series of5–(substituted)aryl–3–(3–coumarinyl)–1–phenyl–2–pyrazolines as novel anti–inflam-matory and analgesic agents, 1682 –Synthesis of [1,2,4]triazolo[1,5–a]pyridinesof potential PGE2 inhibitory properties,1972 – Facile synthesis of bis(4,5–dihy-dro–1H–pyrazole–1–carboxamides) andtheir thio–analogues of potential PGE2inhibitory properties, 2172 – Synthesis,pharmacological screening, quantum chem-ical and in vitro permeability studies ofN–Mannich bases of benzimidazolesthrough bovine cornea, 2307 – Synthesisand pharmacological evaluation of2(3H)–furanones and 2(3H)–pyrrolones,

Page 13: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5143

combining analgesic and anti–inflammatoryproperties with reduced gastrointestinal tox-icity and lipid peroxidation, 2636 –3D–QSAR studies on the inhibitors of AP–1and NF–�B mediated transcriptional activa-tion, 2888 – Synthesis and evaluation of theantioxidant and anti–inflammatory activityof novel coumarin–3–aminoamides andtheir alpha–lipoic acid adducts, 3020 –Synthesis and investigation of anti–inflam-matory activity and gastric ulcerogenicity ofnovel nitric oxide–donating pyrazolinederivatives, 3068 – Synthesis and biologicalevaluation of curcumin–like diarylpen-tanoid analogues for anti–inflammatory,antioxidant and anti–tyrosinase activities,3195 – 1,8–Naphthyridine–3–carboxamidederivatives with anticancer and anti–inflam-matory activity, 3356 – Synthesis and phar-macological evaluation of 1,3,4–oxadiazolebearing bis(heterocycle) derivatives asanti–inflammatory and analgesic agents,3898 – S– and C–nucleosidoquinazoline asnew nucleoside analogs with potential anal-gesic and anti–inflammatory activity, 4249– New pyridone, thioxopyridine, pyra-zolopyridine and pyridine derivatives thatmodulate inflammatory mediators in stimu-lated RAW 264.7 murine macrophage, 4547– Design, synthesis and pharmacologicalscreening of novel nitric oxide donors con-taining 1,5–diarylpyrazolin–3–one as non-toxic NSAIDs, 4622 – Synthesis of6–aminomethyl derivatives of benzopy-ran–4–one with dual biological properties:Anti–inflammatory–analgesic and antimi-crobial, 4896

Anti–inflammatory peptide – Computationalstudy of the electronic structure characteri-zation of a novelanti–inflammatory tripep-tide derived from monocyte locomotioninhibitoryfactor (MLIF)–pentapeptide, 3114

Anti–leishmanial activity –Nitroimidazolyl–1,3,4–thiadiazole–basedanti–leishmanial agents: Synthesis and invitro biological evaluation, 1758

Anti–leishmanial – Anti–oxidant, anti–fungaland anti–leishmanial activities ofn o v e l 3 – [ 4 – ( 1 H – i m i d a z o l – 1 – y l )phenyl]prop–2–en–1–ones, 4654

Anti–leukemia activity – Berbamine deriva-tives: A novel class of compounds foranti–leukemia activity, 3293

Anti–malarial – Design, synthesis and evalu-ation of novel uracil acetamide derivativesas potential inhibitors of Plasmodium falci-parum dUTP nucleotidohydrolase, 678

Anti–microbial activity – Microwave–inducedsynthesis and anti–microbial activities of7,10,11,12–tetrahydrobenzo[c]acridin–8(9H)–one derivatives, 976 – Synthesis and evalua-tion of in vitro anti–microbial and anti–tuber-cular activity of 2–styryl benzimidazoles,4244 – 2–Azetidinone derivatives: Design,synthesis, in vitro anti–microbial, cytotoxicactivities and DNA cleavage study, 5123

Antinociceptive action – Antinociceptive prop-erties of caffeic acid derivatives in mice, 4596

Antinociceptive activity – Synthesis andantinociceptive activity of capsinoid deriva-tives, 3345

Antinociceptive – Synthesis, pharmacologicalevaluation and docking studies of newsulindac analogues, 1959

Anti–osteoporosis – Synthesis, evaluationand 3D QSAR analysis of novelestradiol–RGD octapeptide conjugates withoral anti–osteoporosis activity, 1689

Anti–osteoporotic activity – Synthesis andanti–osteoporotic evaluation of certain3–amino–2–hydroxypropoxyisoflavonederivatives, 3621

Anti–oxidant – Design and synthesis ofazolopyrimidoquinolines, pyrimidoquina-zolines as anti–oxidant, anti–inflammatoryand analgesic activities, 609 – New acyclicnucleosides analogues as potential anal-gesic, anti–inflammatory, anti–oxidant andanti–microbial derived frompyrimido[4,5–b]quinolines, 1427 –Anti–oxidant, anti–fungal and anti–leish-manial activities of novel3–[4–(1H–imida-zol–1–yl) phenyl]prop–2–en–1–ones, 4654

Anti–plasmodial – Design, synthesis andevaluation of novel uracil acetamide deriva-tives as potential inhibitors of Plasmodiumfalciparum dUTP nucleotidohydrolase, 678

Anti–poxvirus agents – Antiviral evaluationof N–amino–1,2,3–triazoles againstCantagalo virus replication in cell culture,3777

Anti–T. cruzi agents – Study of 5–nitroinda-zoles’ anti–Trypanosoma cruzi mode ofaction: Electrochemical behaviour and ESRspectroscopic studies, 1545

Anti–thrombotic – A class of novelN–(3S–1,2,3,4–tetrahydroisoquinoline–3–carbonyl)–l–amino acid derivatives: theirsynthesis, anti–thrombotic activity evalua-tion, and 3D QSAR analysis, 4904

Anti–Trypanosoma cruzi agents –5–Nitro–2–furyl derivative actives againstTrypanosoma cruzi: Preliminary in vivostudies, 3909

Anti–tubercular activity – Synthesis andevaluation of in vitro anti–microbial andanti–tubercular activity of 2–styryl benzim-idazoles, 4244

Anti–tuberculosis agents – Synthesis, opti-mization and structure–activity relation-ships of 3,5–disubstituted isoxazolines asnew anti–tuberculosis agents, 460

Anti–tuberculosis – Synthesis and evaluationof in vitro anti–tuberculosis activity ofN–substituted glycolamides, 289 –Synthesis, anti–tuberculosis activity and3D–QSAR study of amino acid conjugatesof 4–(adamantan–1–yl) group containingquinolines, 2017

Anti–tumor activity – The preparation and invitro antiproliferative activity of phthalimidebased ketones on MDAMB–231 andSKHep–1 human carcinoma cell lines, 2736 –2D– and 3D–QSAR studies on 54 anti–tumorRubiaceae–type cyclopeptides, 3425 – NovelN–(3–carboxyl–9–benzyl–�–carboline–1–yl)ethylamino acids: Synthesis, anti–tumor eval-uation, intercalating determination, 3DQSAR analysis and docking investigation,4153

Anti–tumor agents – Promising carbo-ranylquinazolines for boron neutron capture

therapy: Synthesis, characterization, and invitro toxicity evaluation, 409

Anti–tumor cytotoxicity – Synthesis andanti–tumor activities of some new pyridinesand pyrazolo[1,5–a]pyrimidines, 3519

Anti–tumor – Regioselective synthesis ofd i s p i r o [ 1 H – i n d e n e – 2 , 3 ' – p y r r o l i -dine–2',3"–[3H]indole]–1,2"(1"H)–dionesof potential anti–tumor properties, 91 –Regioselective synthesis and stereochemi-cal structure of anti–tumor activedispiro[3H–indole–3,2'–pyrrolidine–3',3"–piperidine]–2(1H),4"–diones, 1257 – Design,synthesis, and anti–tumor evaluation ofnovel symmetrical bis–benzimidazoles,1808 – Synthesis of[1,2,4]triazolo[1,5–a]pyridines of potentialPGE2 inhibitory properties, 1972 – Studieson chemical structure modification andbiology of a natural product, Gambogic acid(I): Synthesis and biological evaluation ofoxidized analogues of gambogic acid, 2611– Synthesis and biological evaluation of3 , 6 – d i s u b s t i t u t e d[1,2,4]triazolo[3,4–b][1,3,4]thiadiazolederivatives as a novel class of potentialanti–tumor agents, 2776 – Synthesis, char-acterisation and in vitro cytotoxicity studiesof a series of chiral platinum(II) complexesbased on the 2–aminomethylpyrrolidine lig-and: X–ray crystal structure of[ P t C l 2 ( R – d i m e p y r r ) ](R–dimepyrr=N–dimethyl–2(R)–aminomethylpyrrolidine), 2807 –1,8–Naphthyridine–3–carboxamide deriva-tives with anticancer and anti–inflammatoryactivity, 3356 – Synthesis and evaluation ofanti–tumor activities of N4 fatty acyl aminoacid derivatives of 1–�–arabinofuranosyl-cytosine, 3596 – Novel modified steroidderivatives of androstanolone as chemother-apeutic anti–cancer agents, 3936 – Novelcyclic–imide peptidomimetics as aminopep-tidase N inhibitors. Design, chemistry andactivity evaluation. Part I, 4819

Anti–tyrosinase – Synthesis and biologicalevaluation of curcumin–like diarylpen-tanoid analogues for anti–inflammatory,antioxidant and anti–tyrosinase activities,3195

Anti–viral and anti–tumoral activities –Bis–14–membered ring diketal diamines:Synthesis and evaluation of their anti–HIVand anti–tumoral activities, 3138

Anti–VZV activity – Synthesis and anti–VZVactivity of 6–heteroaryl derivatives of tri-cyclic acyclovir and9–{[cis–1',2'–bis(hydroxymethyl)cyclo-prop–1'–yl]methyl}guanine analogues,3313

Antioxidant activity – QSAR study of antiox-idant activity of wine polyphenols, 400 –Synthesis of some N–substituted nitroimi-dazole derivatives as potential antioxidantand antifungal agents, 645 – Cytotoxic,antioxidant activities and structure activityrelationship of some newly synthesized ter-penoidal oxaliplatin analogs, 901 – Newinsights into the antioxidant activity ofhydroxycinnamic acids: Synthesis andphysicochemical characterization of novel

Page 14: Chal Micro

5144 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

halogenated derivatives, 2092 – Synthesis,crystal structure, antioxidant activities andDNA–binding studies of the Ln(III) com-plexes with 7–methoxychromone–3–car-baldehyde–(4'–hydroxy) benzoyl hydra-zone, 2425 – Polycyclic cage structures ascarrier molecules for neuroprotectivenon–steroidal anti–inflammatory drugs,2577 – Copper complexes of pyridine deriv-atives with superoxide scavenging andantimicrobial activities, 3259 – Synthesis,crystal structure, DNA interaction andantioxidant activities of two novelwater–soluble Cu(2�) complexes derivatedfrom 2–oxo–quinoline–3–carbaldehydeSchiff–bases, 4477 – Synthesis of 3,6–dis-ubstituted 7H–1,2,4–triazolo[3,4–b]–1,3,4–thiadiazines as novel analgesic/anti–inflam-matory compounds, 4528 – Synthesis,antimicrobial and antioxidant activities ofsubstituted pyrazoles, isoxazoles, pyrimi-dine and thioxopyrimidine derivatives,4557 – Synthesis, characterization, DNAbinding properties and antioxidant activityof Ln(III) complexes withhesperetin–4–one–(benzoyl) hydrazone,4585 – Synthesis and anti–inflammatoryevaluation of novel angularly or linearlyfused coumarins, 5012

Antioxidant capacity – Blue CrO5 assay: Anovel spectrophotometric method for the eval-uation of the antioxidant and oxidant capacityof various biological substances, 4162

Antioxidant – A theoretical antioxidant phar-macophore for resveratrol, 1644 –Antidyslipidemic and antioxidative activi-ties of 8–hydroxyquinoline derived novelketo–enamine Schiffs bases, 1813 –Synthesis and evaluation of the antioxidantand anti–inflammatory activity of novelcoumarin–3–aminoamides and theiralpha–lipoic acid adducts, 3020 – Synthesisand biological evaluation of curcumin–likediarylpentanoid analogues for anti–inflam-matory, antioxidant and anti–tyrosinaseactivities, 3195 – Antioxidant and antibac-terial studies of arylazopyrazoles and aryl-hydrazonopyrazolones containing coumarinmoiety, 4690 – Captopril and 6–mercaptop-urine: Whose SH possesses higher antioxi-dant ability?, 4841

Antioxidants – QSAR model for predictingradical scavenging activity of di(hetero)ary-lamines derivatives of benzo[b]thiophenes,1952

Antioxidation – Crystal structures, antioxida-tion and DNA binding properties of Dy(III)complexes with Schiff–base ligands derivedfrom 8–hydroxyquinoline–2–carboxalde-hyde and four aroylhydrazines, 5080

Antiparasite – Synthesis, biological evalua-tion and SAR of sulfonamide 4–methoxy-chalcone derivatives with potentialantileishmanial activity, 755

Antiparasitic activity – Lowering of5–nitroimidazole’s mutagenicity: Towardsoptimal antiparasitic pharmacophore, 653

Antiparasitic agents – Synthesis and antipar-asitic and antifungal evaluation of 2'–aryl-substituted–1H,1'H–[2,5']bisbenzimida-zolyl–5–carboxamidines, 2002

Antiparasitic drugs – Scoring function forDNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Antiplasmodial – Synthesis and antiprotozoalactivities of dicationicbis(phenoxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Antiproliferation – Synthesis of2–styrylchromones as a novel class ofantiproliferative agents targeting carcinomacells, 2552

Antiproliferative activity – N–Acylated andN,N'–diacylated imidazolidine–2–thionederivatives and N,N'–diacylated tetrahy-dropyrimidine–2(1H)–thione analogues:Synthesis and antiproliferative activity,1106 – Synthesis and in vitro antiprolifera-tive activity of novel 1–benzhydrylpiper-azine derivatives against human cancer celllines, 1223 – Design, synthesis, and evalua-tion of biphenyl–4–yl–acrylohydroxamicacid derivatives as histone deacetylase(HDAC) inhibitors, 1900 – DNA–targetingpyrroloquinoline–linked butenone and chal-cones: Synthesis and biological evaluation,2854 – 5–Benzylidene–hydantoins:Synthesis and antiproliferative activity onA549 lung cancer cell line, 3471 – Novel2,4,5–trisubstituted oxazole derivatives:Synthesis and antiproliferative activity,3930 – Synthesis ofsubstituted–phenyl–1,2,4–triazol–3–thioneanalogues with modified d–glucopyranosylresidues and their antiproliferative activi-ties, 4716 – Synthesis and serotonin trans-porter activity of sulphur–substituted�–alkyl phenethylamines as a new class ofanticancer agents, 4862

Antiproliferative effect – Novel derivativesof 6–mercaptopurine: Synthesis, characteri-zation and antiproliferative activities ofS–allylthio–mercaptopurines, 541

Antiproliferative – Design, synthesis andstructure–activity relationships of antipro-liferative 1,3–disubstituted urea derivatives,453 – 2,3–Disubstituted–1,4–naphtho-quinones, 12H–benzo[b]phenoth-iazine–6,11–diones and related compounds:Synthesis and Biological evaluation aspotential antiproliferative and antifungalagents, 1086

Antiprotozoal activity – Dialkylamino andnitrogen heterocyclic analogues of hexade-cylphosphocholine and cetyltrimetylammo-nium bromide: Effect of phosphate groupand environment of the ammonium cationon their biological activity, 4970

Antiprotozoal – Synthesis and antiprotozoalactivities of dicationicbis(phenoxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Antiprotozoals – A new series of amodi-aquine analogues modified in the basic sidechain with in vitro antileishmanial andantiplasmodial activity, 5071

Antipsychotic drugs – Molecular propertiesof psychopharmacological drugs determin-

ing non–competitive inhibition of 5–HT3Areceptors, 2667

Antipyretic activities – Synthesis and spec-tral characterization of a new class ofN–(N–methylpiperazinoacetyl)–2,6–diarylpiperidin–4–ones: Antimicrobial, analgesicand antipyretic studies, 577

Antisense – Oligonucleotide–polyamine con-jugates: Influence of length and position of2'–attached polyamines on duplex stabilityand antisense effect, 670

Antithrombin – On designing non–saccha-ride, allosteric activators of antithrombin,2626

Antitrypanosomal – Synthesis and antiproto-zoal activities of dicationic bis(phe-noxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Antitubercular activity – Synthesis, antitu-bercular activity and docking study of novelcyclic azole substituted diphenyl etherderivatives, 492 – Juglone derivatives asantitubercular agents: A rationale for theactivity profile, 2847 – Synthesis and antitu-bercular activity of novel 4–substituted imi-dazolyl–2,6–dimethyl–N3,N5–bisaryl–1,4–dihydropyridine–3,5–dicarboxamides, 3253

Antitubercular agents – A facile synthesis of�,�'–(EE)–bis(benzylidene)–cycloalka-nones and their antitubercular evaluations,1705 – 1,5–Diaryl–2–ethyl pyrrole deriva-tives as antimycobacterial agents: Design,synthesis, and microbiological evaluation,4734

Antitubercular – Synthesis and antimycobac-terial activities of novel 6–nitro-quinolone–3–carboxylic acids, 345 –Synthesis and antitubercular activity of pal-ladium and platinum complexes with fluo-roquinolones, 4107 – Synthesis of new4–isopropylthiazole hydrazide analogs andsome derived clubbed triazole, oxadiazolering systems – A novel class of potentialantibacterial, antifungal and antitubercularagents, 4739

Antituberculotics – QSAR analysis of salicy-lamide isosteres with the use of quantumchemical molecular descriptors, 869

Antitumor activity – 2,3–Disubstituted8–arylamino–3H–imidazo[4,5–g]quinazo-lines: A novel class of antitumor agents, 448– Synthesis and antitumor activity of 6– and2–(1–substituted–thio–4–methylpent–3–enyl)–5,8–dimethoxynaphthalene–1,4–diones,1410 – New transition metal ion complexeswith benzimidazole–5–carboxylic acidhydrazides with antitumor activity, 1500 –Synthesis and in vitro antitumor activity ofnew quinoxaline derivatives, 1579 –Synthesis and characterization of new Pt(II)and Pd(II) complexes with 2–quinolinecar-boxaldehyde selenosemicarbazone:Cytotoxic activity evaluation of Cd(II),Zn(II), Ni(II), Pt(II) and Pd(II) complexeswith heteroaromatic selenosemicarbazones,1623 – Synthesis of novel 3–(aryl)benzoth-ieno[2,3–c]pyran–1–ones from Sonogashiraproducts and intramolecular cyclization:Antitumoral activity evaluation, 1893 –Dideoxy fluoro–ketopyranosyl nucleosides

Page 15: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5145

as potent antiviral agents: Synthesis andbiological evaluation of 2,3– and3,4–dideoxy–3–fluoro–4– and–2–keto–�–d–glucopyranosyl derivativesof N4–benzoyl cytosine, 2696 – Synthesisand antitumor activity of novel dithiocarba-mate substituted chromones, 3687 –Synthesis and antitumoral activity of novelt h i a z o l o b e n z o t r i a z o l e ,thiazoloindolo[3,2–c]quinoline and quinoli-noquinoline derivatives, 3858 –Unsaturated dideoxy fluoro–ketopyranosylnucleosides as new cytostatic agents: A con-venient synthesis of 2,6–dideoxy–3–fluo-ro–4–keto–�–d–glucopyranosyl analoguesof uracil, 5–fluorouracil, thymine, N4–ben-zoyl cytosine and N6–benzoyl adenine,4764

Antitumor agents – A three–step synthesisfrom rebeccamycin of an efficient check-point kinase 1 inhibitor, 2234 – Substitutedquinazolines, part 3. Synthesis, in vitro anti-tumor activity and molecular modelingstudy of certain 2–thieno–4(3H)–quinazoli-none analogs, 2379 – Unusual cellularuptake of cytotoxic4–hydroxymethyl–3–aminoacridine, 4758

Antitumor – Synthesis and in vitro cytotoxicevaluation of novel 3,4,5–trimethoxyphenylsubstituted �–carboline derivatives, 533 –Synthesis and antitumor activity of somenew xanthotoxin derivatives, 2967 – Noveltopoisomerase I–targeting antitumor agentssynthesized from the N,N,N–trimethylam-monium derivative of ARC–111,5H–2,3–dimethoxy–8,9–methylene-dioxy–5–[(2–N,N,N–trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin–6–oneiodide, 3433 – Bromoalkoxyxanthones aspromising antitumor agents: Synthesis,crystal structure and effect on human tumorcell lines, 3830 – Synthesis, characteriza-tion, antimicrobial and antitumor screeningof some diorganotin(IV) complexes of2–[(9H–Purin–6–ylimino)]–phenol, 3981 –Synthesis, characterization and derivatiza-tion of some novel types of mono– andbis–imidazolidineiminothiones and imida-zolidineiminodithiones with antitumor,antiviral, antibacterial and antifungal activi-ties – part I, 4315 – Antitumor and antimy-cobacterial activities of cyclopalladatedcomplexes: X–ray structure of[ P d ( C 2 , N – d m b a ) ( B r ) ( t u ) ](dmba=N ,N–d ime thy lbenzy lamine ,tu=thiourea), 4611 – Novel naphthalimidederivatives as potential apoptosis–inducingagents: Design, synthesis and biologicalevaluation, 4674

Antitumoral activity – Novel trans–dichlori-doplatinum(II) complexes with 3– and4–acetylpyridine: Synthesis, characteriza-tion, DFT calculations and cytotoxicity,1921 – Palladium(II) complexes withR2edda–derived ligands. Part II. Synthesis,characterization and in vitro antitumoralstudies of R2eddip esters and palladium(II)complexes, 3452

Antitumoral – Hydroxychalcones induceapoptosis in B16–F10 melanoma cells viaGSH and ATP depletion, 1630

Antitumour activity – Antitumour activity ofnovel 1,10–phenanthroline and5–amino–1,10–phenanthroline derivatives,2720

Antitumour agents – Synthesis, kinaseinhibitory potencies and in vitro antiprolif-erative activity of isoindigo and 7'–aza-isoindigo derivatives substituted bySonogashira cross–coupling, 2705

Antitumour drugs – Towards an efficientprodrug of the alkylating metabolitemonomethyltriazene: Synthesis and stabili-ty of N–acylamino acid derivatives of tri-azenes, 1049

Antitumour – Reactivity of isothiazolonesand isothiazolone–1–oxides in the inhibi-tion of the PCAF histone acetyltransferase,4855

Antiviral activity – Synthesis and in vitroanti–HIV evaluation of a new series of6–arylmethyl–substituted S–DABOs aspotential non–nucleoside HIV–1 reversetranscriptase inhibitors, 1016 – Anti–HIVevaluation of benzo[d]isothiazole hydra-zones, 1801 – Synthesis, antimicrobial andantiviral evaluation of substituted imidazolederivatives, 2347 – Synthesis and biologicalevaluation of abietic acid derivatives, 2468– Synthesis, antiviral and anticancer activi-ty of some novel thioureas derivedfromN–(4–nitro–2–phenoxyphenyl)–methane-sulfonamide, 3591 – Synthesis of newacridines and hydrazones derived fromcyclic �–diketone for cytotoxic and antivi-ral evaluation, 3680 – Synthesis and antivi-ral activity of new pyrazole and thiazolederivatives, 3746 – Synthesis and anti–HIVactivity evaluation of 2–(4–(naph-thalen–2–yl)–1,2,3–thiadiazol–5–ylthio)–N–acetamides as novel non–nucleosideHIV–1 reverse transcriptase inhibitors,4648 – Synthesis and antiviral activity of�–carboline derivatives bearing a substitut-ed carbohydrazide at C–3 against poliovirusand herpes simplex virus (HSV–1), 4695

Antiviral agent – Cyclic phosphoramidates asprodrugs of 2'–C–methylcytidine, 3765

Antiviral evaluation – Synthesis andanti–HSV–1 evaluation of some pyrazolesand fused pyrazolopyrimidines, 3285

Antiviral – Synthesis, HIV–RT inhibitoryactivity and SAR of1–benzyl–1H–1,2,3–triazole derivatives ofcarbohydrates, 373 – Structure–activityrelationships for dipeptide prodrugs of acy-clovir: Implications for prodrug design,2339 – Dideoxy fluoro–ketopyranosylnucleosides as potent antiviral agents:Synthesis and biological evaluation of 2,3–and 3,4–dideoxy–3–fluoro–4– and–2–keto–�–d–glucopyranosyl derivativesof N4–benzoyl cytosine, 2696 – Synthesis,characterization and derivatization of somenovel types of mono– and bis–imidazo-lidineiminothiones and imidazolidineimin-odithiones with antitumor, antiviral, anti-bacterial and antifungal activities – part I,4315 – Unsaturated dideoxy fluoro–ketopy-ranosyl nucleosides as new cytostaticagents: A convenient synthesis of2,6–dideoxy–3–fluoro–4–keto–�–d–glu-

copyranosyl analogues of uracil, 5–fluo-rouracil, thymine, N4–benzoyl cytosine andN6–benzoyl adenine, 4764

B��–Tocopherol – Blue CrO5 assay: A novel

spectrophotometric method for the evalu-ation of the antioxidant and oxidantcapacity of various biological substances,4162

��–Triple–helix peptides – Circular dichro-ism studies of type III collagen mimeticpeptides with anti– or pro–aggregantactivities on human platelets, 2643

AAnxiolytics/antidepressants – Synthesis and

preliminary pharmacological evaluation ofimidazo[2,1–f]purine–2,4–dione deriva-tives, 4288

AP–1 – 3D–QSAR studies on the inhibitors ofAP–1 and NF–�B mediated transcriptionalactivation, 2888

Apoptosis inducer – Studies on chemicalstructure modification and biology of a nat-ural product, Gambogic acid (I): Synthesisand biological evaluation of oxidized ana-logues of gambogic acid, 2611

Apoptosis – Synthesis, cytotoxicity and apop-tosis of naphthalimide polyamine conju-gates as antitumor agents, 393 – Novelderivatives of 6–mercaptopurine: Synthesis,characterization and antiproliferative activi-ties of S–allylthio–mercaptopurines, 541 –Discovery of a new family ofbis–8–hydroxyquinoline substituted benzy-lamines with pro–apoptotic activity in can-cer cells: Synthesis, structure–activity rela-tionship, and action mechanism studies, 558– Hydroxychalcones induce apoptosis inB16–F10 melanoma cells via GSH and ATPdepletion, 1630 – Highly twisted adamantylarotinoids: Synthesis, antiproliferativeeffects and RXR transactivation profiles,2434 – Synthesis, NMR characterizationand in vitro antitumor evaluation of newaminophosphonic acid diesters, 3363 –Physicochemical properties and membraneinteractions of anti–apoptotic derivatives2–(4–fluorophenyl)–3–(pyridin–4–yl)imi-dazo[1,2–a]pyridine depending on thehydroxyalkylamino side chain length andconformation: An NMR and ESR study,3509 – Novel naphthalimide derivatives aspotential apoptosis–inducing agents:Design, synthesis and biological evaluation,4674 – Synthesis and serotonin transporteractivity of sulphur–substituted �–alkylphenethylamines as a new class of anti-cancer agents, 4862

Apoptotic – Synthesis, Raman, FT–IR, NMRspectroscopic characterization, antimicro-bial activity, cytotoxicity and DNA bindingof new mixed aza–oxo–thia macrocycliccompounds, 4681

Apotosis – Synthesis and biological evalua-tion of novel symmetry bis–enediynes, 35

Arachidonic acid metabolism – Design, syn-thesis and evaluation of tetrahydropyranbased COX–1/–2 inhibitors, 1278

Page 16: Chal Micro

5146 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Arachidonyl – Synthesis and pharmacologi-cal evaluation of sulfamide–based ana-logues of anandamide, 4889

Ara–C derivatives – Synthesis and evaluationof anti–tumor activities of N4 fatty acylamino acid derivatives of 1–�–arabinofura-nosylcytosine, 3596

Ara–C – Synthesis and evaluation ofanti–tumor activities of N4 fatty acyl aminoacid derivatives of 1–�–arabinofuranosyl-cytosine, 3596

Arborescidine – Antiproliferative activity ofarborescidine alkaloids and derivatives,3810

ARC–111 – Novel topoisomerase I–targetingantitumor agents synthesized from theN,N,N–trimethylammonium derivative ofARC–111, 5H–2,3–dimethoxy–8,9–methyl-enedioxy–5–[(2–N,N,N–trimethylammoni-u m ) e t h y l ] d i b e n z o [ c , h ] [ 1 , 6 ] n a p h -thyridin–6–one iodide, 3433

Arecoline derivatives – Synthesis and phar-macological evaluation of novelN–alkyl/aryl substituted thiazolidinonearecoline analogues as muscarinic receptor1 agonist in Alzheimer’s dementia models,4848

Arginine vasopressin (AVP) analogues –Arginine vasopressin and its analogues –The influence of position 2 modificationwith 3,3–diphenylalanine enantiomers.Highly potent V2 agonists, 2862

Aromatase inhibitors – An efficient steroidpharmacophore–based strategy to identifynew aromatase inhibitors, 4121

Aroylpropionic acid – Aroylpropionic acidbased 2,5–disubstituted–1,3,4–oxadiazoles:Synthesis and their anti–inflammatory andanalgesic activities, 2372

Artemia salina Leach. – Improved synthesisof seven aromatic Baylis–Hillman adducts(BHA): Evaluation against Artemia salinaLeach. and Leishmania chagasi, 1726

Artemisinin – Antimalarial pharmacodynam-ics of chalcone derivatives in combinationwith artemisinin against Plasmodium falci-parum in vitro, 3388

Artificial cleavage activity – Synthesis andcharacterization of dinuclear macrocycliccobalt(II), copper(II) and zinc(II) complex-es derived from2,2,2',2'–S,S[bis(bis–N,N–2–thiobenzimida-zolyloxalato–1,2–ethane)]: DNA bindingand cleavage studies, 834

Artificial neural networks – Prediction ofmilk/plasma concentration ratios of drugsand environmental pollutants, 2452

Aryl alkanol piperazine derivatives –Quantitative structure–activity relationshipanalysis of aryl alkanol piperazine deriva-tives with antidepressant activities, 4367

Aryl alkenyl amides/imines – Quantitativestructure–activity relationship (QSAR) ofaryl alkenyl amides/imines for bacterialefflux pump inhibitors, 229

Arylalkylpiperazines – Synthesis and prelim-inary pharmacological evaluation of imida-zo[2,1–f]purine–2,4–dione derivatives, 4288

Aryl–amines – Known drug space as a metricin exploring the boundaries of drug–likechemical space, 5006

Aryl–nitro – Known drug space as a metric inexploring the boundaries of drug–likechemical space, 5006

Arylpiperazine – Synthesis and serotoninreceptor activity of the arylpiperazinealkyl/propoxy derivatives of new azatricy-cloundecanes, 152 – Application of desir-ability–based multi(bi)–objective optimiza-tion in the design of selective arylpiperazinederivates for the 5–HT1A serotonin receptor,5045

Arylsulfonylmethyl group – Lowering of5–nitroimidazole’s mutagenicity: Towardsoptimal antiparasitic pharmacophore, 653

Ascorbate – Blue CrO5 assay: A novel spec-trophotometric method for the evaluation ofthe antioxidant and oxidant capacity of var-ious biological substances, 4162

Aspartyl–protease – 3D–QSARCoMFA/CoMSIA models based on theoret-ical active conformers ofHOE/BAY–793analogs derived from HIV–1 proteaseinhibitor complexes, 4344

Asteraceae – Structure–activity relationshipof seco–tanapartholides isolated fromAchillea falcata for inhibition of HaCaT cellgrowth, 3794

Asthma – A series of 1, 2–coupled indanedimers with mast cell stabilisation andsmooth muscle relaxation properties, 5018

Atovaquone – Synthesis and antimalarialactivity of new atovaquone derivatives, 4778

ATP – Hydroxychalcones induce apoptosis inB16–F10 melanoma cells via GSH and ATPdepletion, 1630

ATP overproduction – Theporphyrin–fullerene nanoparticles to pro-mote the ATP overproduction in myocardi-um: 25Mg2�–magnetic isotope effect, 1554

Aurantiamide acetate – Rare dipeptide andurea derivatives from roots of Moringaoleifera as potential anti–inflammatory andantinociceptive agents, 432

Aurantiamide derivatives – Design and syn-thesis of new N–(fluorenyl–9–methoxycar-bonyl) (Fmoc)–dipeptides as anti–inflam-matory agents, 1933

Aurone – Design, synthesis and AChEinhibitory activity of indanone and auronederivatives, 7

Azalides – Novel ureas and thioureas of15–membered azalides with antibacterialactivity against key respiratory pathogens,3459

Azatricycloundecane – Synthesis and sero-tonin receptor activity of the arylpiperazinealkyl/propoxy derivatives of new azatricy-cloundecanes, 152

Azetidin–2–ones – Synthesis and evaluationof some new benzimidazole derivatives aspotential antimicrobial agents, 2294

Azetidinones – Synthesis and anti–inflamma-tory activity of newer quinazolin–4–onederivatives, 83

Aziridine – Aziridine alkaloids as potentialtherapeutic agents, 3373

Azole – New azoles with potent antifungalactivity: Design, synthesis and moleculardocking, 4218

Azomethine ylide – A facile synthesis andantimycobacterial evaluation of novel

spiro–pyrido–pyrrolizines and pyrrolidines,3821

Azomethine ylides – Regioselective synthesisof dispiro[1H–indene–2,3'–pyrroli-dine–2',3"–[3H]indole]–1,2"(1"H)–dionesof potential anti–tumor properties, 91 –Regioselective synthesis and antimicrobialscreening of novel ketocarbazolodispiropy-rrolidine derivatives, 959 – Regioselectivesynthesis and stereochemical structure ofanti–tumor active dispiro[3H–indole–3,2'–pyrrolidine–3',3"–piperidine]–2(1H),4"–diones, 1257

B��2 Adrenoceptor agonist – Synthesis, phar-

macological and in silico evaluation of1–(4–di–hydroxy–3,5–dioxa–4–borabicy-clo[4.4.0]deca–7,9,11–trien–9–yl)–2–(tert–butylamino)ethanol, a compounddesigned to act as a ��2 adrenoceptor ago-nist, 2840

��3–Adrenergic receptor – Discovery of novelacetanilide derivatives as potent andselective ��3–adrenergic receptor agonists,2533

Bacillus thuringiensis – Synthesis and anti-bacterial activity of some new heterocyclesincorporating phthalazine, 4448

Bacteria – Synthesis and evaluation of anti-bacterial activities of andrographolide ana-logues, 2936

Balance of correlations – QSPR modelingbioconcentration factor (BCF) by balance ofcorrelations, 2544

Baylis–Hillman adducts – Improved synthe-sis of seven aromatic Baylis–Hillmanadducts (BHA): Evaluation against Artemiasalina Leach. and Leishmania chagasi,1726

bcl–2 – Oligonucleotide–polyamine conju-gates: Influence of length and position of2'–attached polyamines on duplex stabilityand antisense effect, 670

BCS system – The structure–bioavailabilityapproach in antifungal agents, 1978

Benzal hydrazone – Synthesis and analgesicand anti–inflammatory activities 6–substi-tuted–3(2H)–pyridazinone–2–acetyl–2–(p–substituted/nonsubstituted benzal)hydra-zone derivatives, 3760

Benzamides – Synthesis of benzamide deriv-atives of anacardic acid and their cytotoxicactivity, 2711

Benzene–1,4–dicarboxaldehyde – Synthesis,characterization, antiamoebic activity andtoxicity of novel bisdioxazole derivatives,4747

Benzimidazole analogues – Synthesis and in vitro cysticidal activity of new benzimi-dazole derivatives, 1794

Benzimidazole derivatives – Synthesis and invitro antimicrobial activity of some novelsubstituted benzimidazole derivatives hav-ing potent activity against MRSA, 1024

Benzimidazole macrocylic complexes –Synthesis and characterization of dinuclearmacrocyclic cobalt(II), copper(II) andzinc(II) complexes derived from2,2,2',2'–S,S[bis(bis–N,N–2–thiobenzimida-

Page 17: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5147

zolyloxalato–1,2–ethane)]: DNA bindingand cleavage studies, 834

Benzimidazole – Design, synthesis and anti-bacterial activity of novel actinonin deriva-tives containing benzimidazole heterocy-cles, 2202 – Synthesis, pharmacologicalscreening, quantum chemical and in vitropermeability studies of N–Mannich bases ofbenzimidazoles through bovine cornea,2307 – Synthesis and antinociceptive activ-ities of some pyrazoline derivatives, 2606 –Synthesis, physicochemical properties andantimicrobial activity of some new benzim-idazole derivatives, 4028

Benznidazole – Synthesis and in vitro tri-chomonicidal, giardicidal and amebicidalactivity ofN–acetamide(sulfonamide)–2–methyl–4–nitro–1H–imidazoles, 2975

Benzo[b]thiophene – Synthesis and pharma-cological evaluation of 2–substitutedbenzo[b]thiophenes as anti–inflammatoryand analgesic agents, 1718

Benzo[b]thiophenes – QSAR model for pre-dicting radical scavenging activity of di(het-ero)arylamines derivatives of benzo[b]thio-phenes, 1952 – Synthesis of novel3–(aryl)benzothieno[2,3–c]pyran–1–onesfrom Sonogashira products and intramolec-ular cyclization: Antitumoral activity evalu-ation, 1893

Benzo[d]isothiazole hydrazones – Anti–HIVevaluation of benzo[d]isothiazole hydra-zones, 1801

Benzo[d]isothiazol–3–one benzenesulfon-amides – Hybrid molecules between ben-zenesulfonamides and active antimicrobialbenzo[d]isothiazol–3–ones, 2741

Benzo[d]isothiazol–3–one derivatives –Anti–HIV evaluation of benzo[d]isothiazolehydrazones, 1801

Benzo[d]oxazol–2(3H)–one derivatives –Substituted benzo[d]oxazol–2(3H)–onederivatives with preference for the �1 bind-ing site, 124

Benzofuran – Synthesis and antimicrobialevaluation of 1–(benzofuran–2–yl)–4–nitro–3–arylbutan–1–ones and 3–(benzofu-ran–2–yl)–4,5–dihydro–5–aryl–1–[4–(aryl)–1,3–thiazol–2–yl]–1H–pyrazoles, 2632

Benzofuranes – Diversity–oriented synthesisof furo[3,2–f]chromanes with antimycobac-terial activity, 2497

Benzofurans – Convenient synthesis andantimicrobial evaluation of some novel2–substituted–3–methylbenzofuran deriva-tives, 3637 – Stereoselective synthesis andantimicrobial activity of benzofuran–based(1E)–1–(piperidin–1–yl)–N2–arylamidra-zones, 4985

Benzofurobenzopyrone – Tetrahydrobenzo–and benzofurobenzopyrones as a new classof potential photoreagents toward DNA, 18

Benzoimidazo[1,2–c]quinazoline – Synthesisand affinity to DNA of phenylbenzoimida-zoles and benzoimidazo[1,2–c]quinazo-lines, 3305

Benzophenone – Design, synthesis, andevaluation of benzophenone derivatives asnovel acetylcholinesterase inhibitors,1341

Benzophenones – Natural polyprenylatedbenzophenones inhibiting cysteine and ser-ine proteases, 1230 – Synthesis and antiox-idant potential of novel synthetic benzophe-none analogues, 2724

Benzopyran derivatives – QSAR modellingof pancreatic �–cell KATP channel openersR/S–3,4–dihydro–2,2–dimethyl–6–halo–4–( s u b s t i t u t e dphenylaminocarbonylamino)–2H–1–ben-zopyrans using MLR–FA techniques, 359

Benzothiazepines – Mechanistic aspects ofbenzothiazepines: A class of antiarrhythmicdrugs, 1

Benzothiazines – Synthesis and antimalarialactivity of pyrazolo and pyrimido benzoth-iazine dioxide derivatives, 1303

Benzothiazoles – Enaminonitrile in hetero-cyclic synthesis: Synthesis and antimicro-bial evaluation of some new pyrazole, isox-azole and pyrimidine derivatives incorpo-rating a benzothiazole moiety, 4813

Benzothieno[2,3–c]pyran–1–ones –Synthesis of novel 3–(aryl)benzoth-ieno[2,3–c]pyran–1–ones from Sonogashiraproducts and intramolecular cyclization:Antitumoral activity evaluation, 1893

Benzotriazole – Design, synthesis, and anti-fungal activity of triazole and benzotriazolederivatives, 3064

Benzotriazoles – Synthesis and antitumoralactivity of novel thiazolobenzotriazole, thi-azoloindolo[3,2–c]quinoline and quinolino-quinoline derivatives, 3858

Benzoxazole – Preparation and in vitro evalu-ation of benzylsulfanyl benzoxazole deriva-tives as potential antituberculosis agents,2286 – Synthesis and antinociceptive activ-ities of some pyrazoline derivatives, 2606

Benzoxazoles – Synthesis, biological evalua-tion and 2D–QSAR analysis of benzoxa-zoles as antimicrobial agents, 501

Benzylamine – Discovery of a new family ofbis–8–hydroxyquinoline substituted benzy-lamines with pro–apoptotic activity in can-cer cells: Synthesis, structure–activity rela-tionship, and action mechanism studies, 558

Benzylidene derivatives – Synthesis, antimi-crobial and cytotoxic activities of some5–arylidene–4–thioxo–thiazolidine–2–ones,2038

Berbamine derivatives – Berbamine deriva-tives: A novel class of compounds foranti–leukemia activity, 3293

Beta–carboline – Antiproliferative activity ofarborescidine alkaloids and derivatives,3810

Biased screen – Design of novel aminopyrro-lidine factor Xa inhibitors from a screeninghit, 2787

Bicyclic ��–lactam – Large ring 1,3–bridged2–azetidinones: Experimental and theo-retical studies, 2071

Bicyclo–octyl ester – Antiplasmodial andantitrypanosomal activities of aminobicy-clo[2.2.2]octyl �–aminoalkanoates, 736

Bifunctional alkylating agents – To deter-mine the cytotoxicity of chlorambucil andone of its nitro–derivatives, conjugated toprasterone and pregnenolone, towards eighthuman cancer cell–lines, 2944

Biginelli dihydropyrimidines – NovelBiginelli dihydropyrimidines with potentialanticancer activity: A parallel synthesis andCoMSIA study, 4192

Biginelli dihydropyrimidinones –N 1 – A l k y l a t e d3,4–dihydropyrimidine–2(1H)–ones:Convenient one–pot selective synthesis andevaluation of their calcium channel block-ing activity, 1997

Biginelli reaction – Synthesis and pharmaco-logical investigation of 3–(substituted1–pheny le thanone )–4–( subs t i t u t edphenyl)–1, 2, 3, 4–tetrahydropyrimi-dine–5–carboxylates, 3645

Binding constant – Synthesis, spectroscopiccharacterization, X–ray structure and evalu-ation of binding parameters of new triorgan-otin(IV) dithiocarboxylates with DNA,3986

Binding – Structure–activity relationship ofdopaminergic halogenated 1–benzyl–tetrahy-droisoquinoline derivatives, 4616

Binuclear platinum(II) complexes –Synthesis, characterization and antitumoractivity of new type binuclear platinum(II)complexes, 2322 – Synthesis, cytotoxicityand DNA–binding levels of new type binu-clear platinum(II) complexes, 4772

Bioactive conformation – Studies towardsthe identification of putative bioactive con-formation of potent vasodilator arylideneN–acylhydrazone derivatives, 4004

Bioactive diversity – Novel 4H–1,3,4–oxadi-azin–5(6H)–ones with hydrophobic andlong alkyl chains: Design, synthesis, andbioactive diversity on inhibition ofmonoamine oxidase, chitin biosynthesis andtumor cell, 2113

Bioactivity – Regioselective synthesis andantimicrobial screening of novel ketocar-bazolodispiropyrrolidine derivatives, 959

Bioanalysis – Didanosine ester prodrugs:Synthesis, albumin binding properties andpharmacokinetic studies in rats, 3874

Bioavailability – The structure–bioavailabili-ty approach in antifungal agents, 1978

Biochemical and immunohistochemicalstudies – Synthesis, characterization andantidiabetic properties of N1–2,4–dihydrox-ybenzylidene–N4–2–hydroxybenzylidene–S–methyl–thiosemicarbazidato–oxovanadi-um(IV), 818

Biocides – Synthesis and antimicrobial prop-erties of polymerizable quaternary ammoni-ums, 3201

Bioconcentration factor – QSPR modelingbioconcentration factor (BCF) by balance ofcorrelations, 2544

Biofilm – Synthesis and evaluation of antibac-terial activities of andrographolide ana-logues, 2936

Bioinorganic – Metals in anticancer therapy:Copper(II) complexes as inhibitors of the20S proteasome, 4353

Biological activities – Synthesis, analgesic,anti–inflammatory and antimicrobial stud-ies of 2,4–dichloro–5–fluorophenyl con-taining thiazolotriazoles, 827

Biological activity – Synthesis, characteriza-tion and in vitro antiproliferative activities

Page 18: Chal Micro

5148 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

of new 13–cis–retinoyl ferrocene deriva-tives, 2572 – Synthesis of some novelbioactive 4–oxy/thio substituted–1H–pyra-zol–5(4H)–ones via efficient cross–Claisencondensation, 3852 – Biological activitystudies on metal complexes of novel triden-tate Schiff base ligand. Spectroscopic andthermal characterization, 4801

Biological evaluation – Synthesis and biolog-ical evaluation of novel luteolin derivativesas antibacterial agents, 908 – In vitro and invivo antitumor activity of platinum(II) com-plexes with thiosemicarbazones derivedfrom 2–formyl and 2–acetyl pyridine andcontaining ring incorporated at N(4)–posi-tion: Synthesis, spectroscopic study andcrystal structure of platinum(II) complexeswith thiosemicarbazones, potential anti-cancer agents, 1296 – Synthesis and biolog-ical evaluation of a novel series of 1,5–ben-zothiazepine derivatives as potential antimi-crobial agents, 2815

Biological – Synthesis, spectral characteriza-tion, in–vitro microbiological evaluationand cytotoxic activities of novel macro-cyclic bis hydrazone, 3552

Biotin – Targeting cancer cells withbiotin–dendrimer conjugates, 862

Biotransformation – Condensed 1,4–dihy-dropyridines with various esters and theircalcium channel antagonist activities, 2052

Bis(2–propen–1–ones) – Facile synthesis ofbis(4,5–dihydro–1H–pyrazole–1–carbox-amides) and their thio–analogues of poten-tial PGE2 inhibitory properties, 2172

Bis(3–aryl–4,5–dihydro–1H–pyrazole–1–carboxamides) – Facile synthesis ofbis(4,5–dihydro–1H–pyrazole–1–carbox-amides) and their thio–analogues of poten-tial PGE2 inhibitory properties, 2172

Bis(3–aryl–4,5–dihydro–1H–pyrazole–1–thiocarboxamides) – Facile synthesis ofbis(4,5–dihydro–1H–pyrazole–1–carbox-amides) and their thio–analogues of poten-tial PGE2 inhibitory properties, 2172

Bis(heterocycle) – Synthesis and pharmaco-logical evaluation of 1,3,4–oxadiazole bear-ing bis(heterocycle) derivatives asanti–inflammatory and analgesic agents,3898

Bisammoniums – Enhanced activity of fluori-nated quaternary ammonium surfactantsagainst Pseudomonas aeruginosa, 1615

Bisbenzimidazoles – Synthesis and antipara-sitic and antifungal evaluation of 2'–aryl-substituted–1H,1'H–[2,5']bisbenzimida-zolyl–5–carboxamidines, 2002

Bisbenzylisoquinoline alkaloid – Berbaminederivatives: A novel class of compounds foranti–leukemia activity, 3293

Bischalcone – Bis–pyrazolines: Synthesis,characterization and antiamoebic activity asinhibitors of growth of Entamoeba histolyt-ica, 426

Bischier–Napieralski – The synthesis ofN–phenoxyethyl–1–substituted–1,2,3,4–tetrahydroisoquinolines and their �1–adreno-ceptor blocking activity, 1271

Bisdioxazoles – Synthesis, characterization,antiamoebic activity and toxicity of novelbisdioxazole derivatives, 4747

Bishydrazones – Synthesis and anticonvul-sant activity of some new bishydrazonesderived from 3,4–dipropyloxythiophene,3672

Bis–diketal diamine macrocycles –Bis–14–membered ring diketal diamines:Synthesis and evaluation of their anti–HIVand anti–tumoral activities, 3138

Bis–enediynes – Synthesis and biologicalevaluation of novel symmetrybis–enediynes, 35

Bis–hydroxyquinoline – Discovery of a newfamily of bis–8–hydroxyquinoline substitut-ed benzylamines with pro–apoptotic activi-ty in cancer cells: Synthesis,structure–activity relationship, and actionmechanism studies, 558

Bis–imidazolidineiminothiones – Synthesis,characterization and derivatization of somenovel types of mono– and bis–imidazo-lidineiminothiones and imidazolidineimin-odithiones with antitumor, antiviral, anti-bacterial and antifungal activities – part I,4315

Bis–imides – Synthesis, antiarrhythmic andanticoagulant activities of novel thiazoloderivatives from methyl2–(thiazol–2–ylcarbamoyl)acetate, 725

Bis–Pyrazolines – Bis–pyrazolines:Synthesis, characterization and antiamoebicactivity as inhibitors of growth ofEntamoeba histolytica, 426

Bis–pyridinium oximes – In–vitro regenera-tion of sarin inhibited electric eel acetyl-cholinesterase by bis–pyridinium oximesbearing xylene linker, 1326 – Synthesis andevaluation of novel bis–pyridinium oximesas reactivators of DFP–inhibited acetyl-cholinesterase, 1335

Bis–quinolines – Phase transfer catalyzedsynthesis of bis–quinolines: Antileishmanialactivity in experimental visceral leishmani-asis and in vitro antibacterial evaluation,845

Bisphosphonates – Acyclic nucleoside bis-phosphonates: Synthesis and properties ofchiral 2–amino–4,6–bis[(phospho-nomethoxy)alkoxy]pyrimidines, 2408

Bisthiazolidinones – Synthesis, characteriza-tion and in vitro antimicrobial activity ofnovel 2–thioxo–4–thiazolidinones and4,4'–bis(2–thioxo–4–thiazolidinone–3–yl)diphenylsulfones, 4148

BK–channels activity – Application of genet-ic algorithm–support vector machine(GA–SVM) for prediction of BK–channelsactivity, 5023

Blind docking – CoMFA, LeapFrog and blinddocking studies on sulfonanilide derivativesacting as selective aromatase expressionregulators, 3445

Blood glucose lowering effect – Synthesisand blood glucose lowering effect of novelpyridazinone substituted benzenesulfony-lurea derivatives, 2673

Blood–brain barrier permeability –Polycyclic cage structures as carrier mole-cules for neuroprotective non–steroidalanti–inflammatory drugs, 2577

BM 212 – 1,5–Diaryl–2–ethyl pyrrole deriva-tives as antimycobacterial agents: Design,

synthesis, and microbiological evaluation,4734

��–Amyloid – Synthesis and activity of fibril-logenesis peptide inhibitors related to the17–21 ��–amyloid sequence, 179

��–Carboline – Synthesis and in vitro cyto-toxic evaluation of novel3,4,5–trimethoxyphenyl substituted��–carboline derivatives, 533

BNCT – Promising carboranylquinazolinesfor boron neutron capture therapy:Synthesis, characterization, and in vitro tox-icity evaluation, 409

��–Elimination reaction – Unsaturateddideoxy fluoro–ketopyranosyl nucleo-sides as new cytostatic agents: A conven-ient synthesis of 2,6–dideoxy–3–fluo-ro–4–keto–��–d–glucopyranosyl analoguesof uracil, 5–fluorouracil, thymine, N4–ben-zoyl cytosine and N6–benzoyl adenine,4764

��–Hematin – Synthesis and antimalarialactivity of pyrazolo and pyrimido ben-zothiazine dioxide derivatives, 1303

��–Ketone aldehyde – Synthesis and antibac-terial evaluation of novel 4–alkyl substi-tuted phenyl ��–aldehyde ketone deriva-tives, 1737

Bond–dissociation enthalpy – Melatonin:Quantum–chemical and biochemical inves-tigation of antioxidant activity, 2834

Bon–naharu – Anti–genotoxic hydrazidefrom Crinum defixum, 2754

Boric acid – A novel spectrophotometricmethod for the determination of amino-phylline with boric acid in pharmaceuticaland mixed serum samples, 1452

Boron – Synthesis, pharmacological and insilico evaluation of1–(4–di–hydroxy–3,5–dioxa–4–borabicy-clo[4.4.0]deca–7,9,11–trien–9–yl)–2–(tert–butylamino)ethanol, a compound designedto act as a �2 adrenoceptor agonist, 2840

Bovine hemoglobin – Studies on the interac-tion of caffeine with bovine hemoglobin,2100

Bovine seminal ribonuclease – Mapping theribonucleolytic active site of bovine seminalribonuclease. The binding of pyrimidinylphosphonucleotide inhibitors, 4496

BPH – Self organizing molecular field analy-sis on a series of human 5�–reductaseinhibitors: Unsaturated 3–carboxysteroid,4920

Brain and tumor imaging – Synthesis of[11C]FEDAA1106 as a new PET imagingprobe of peripheral benzodiazepine receptorexpression, 2748

BrdU–cell cycle – Dideoxy fluoro–ketopyra-nosyl nucleosides as potent antiviral agents:Synthesis and biological evaluation of 2,3–and 3,4–dideoxy–3–fluoro–4– and–2–keto–�–d–glucopyranosyl derivativesof N4–benzoyl cytosine, 2696

Breast cancer – An efficient steroid pharma-cophore–based strategy to identify new aro-matase inhibitors, 4121

Breast carcinoma – The preparation and invitro antiproliferative activity of phthalim-ide based ketones on MDAMB–231 andSKHep–1 human carcinoma cell lines, 2736

Page 19: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5149

BR–AEA – Synthesis, pharmacological and insilico evaluation of1–(4–di–hydroxy–3,5–dioxa–4–borabicy-clo[4.4.0]deca–7,9,11–trien–9–yl)–2–(tert–butylamino)ethanol, a compound designedto act as a �2 adrenoceptor agonist, 2840

Broad–spectrum – Synthesis, Raman, FT–IR,NMR spectroscopic data and antimicrobialactivity of mixed aza–oxo–thia macrocycliccompounds, 365

Bromoalkoxyxanthone –Bromoalkoxyxanthones as promising anti-tumor agents: Synthesis, crystal structureand effect on human tumor cell lines, 3830

Bromohydroxycinnamic acids – Newinsights into the antioxidant activity ofhydroxycinnamic acids: Synthesis andphysicochemical characterization of novelhalogenated derivatives, 2092

Broth dilution assay – Synthesis of new4–isopropylthiazole hydrazide analogs andsome derived clubbed triazole, oxadiazolering systems – A novel class of potentialantibacterial, antifungal and antitubercularagents, 4739

Butenolide – Synthesis of new chiral 2,5–dis-ubstituted 1,3,4–thiadiazoles possessing�–butenolide moiety and preliminary evalu-ation of in vitro anticancer activity, 3340

Butyrylcholinesterase inhibitors –Synthesis, biological evaluation and molec-ular modeling of oxoisoaporphine andoxoaporphine derivatives as new dualinhibitors of acetylcholinesterase/butyryl-cholinesterase, 2523

CC log P – Adamantane derivatives of thia-

zolyl–N–substituted amide, as possiblenon–steroidal anti–inflammatory agents,1198

C2–Symmetric diol – 3D–QSARCoMFA/CoMSIA models based on theoret-ical active conformers ofHOE/BAY–793analogs derived from HIV–1 proteaseinhibitor complexes, 4344

Caffeic acid derivatives – Antinociceptiveproperties of caffeic acid derivatives inmice, 4596

Caffeine – Studies on the interaction of caf-feine with bovine hemoglobin, 2100

Calcium antagonistic activity – Condensed1,4–dihydropyridines with various estersand their calcium channel antagonist activi-ties, 2052

Calf thymus DNA binding propeties –Crystal structures, antioxidation and DNAbinding properties of Dy(III) complexeswith Schiff–base ligands derived from8–hydroxyquinoline–2–carboxaldehydeand four aroylhydrazines, 5080

Calpain inhibitor – Design and synthesis ofcalpain inhibitory 6–pyridone 2–carboxam-ide derivatives, 1331

Cancer chemoprevention – New cyclopen-tane derivatives as inhibitors of steroidmetabolizing enzymes AKR1C1 andAKR1C3, 2563

Cancer – Synthesis and biological evaluationof benzenesulfonamide–substituted

4–(6–alkylpyridin–2–yl)–5–(quinox-alin–6–yl)imidazoles as transforminggrowth factor–� type 1 receptor kinaseinhibitors, 568 – Steroidal lactones asinhibitors of 17�–hydroxysteroid dehydro-genase type 5: Chemical synthesis, enzymeinhibitory activity, and assessment of estro-genic and androgenic activities, 632

Cancer targeting – Targeting cancer cellswith biotin–dendrimer conjugates, 862

Candida albicans – Photodynamic inactiva-tion of Candida albicans sensitized by tri–and tetra–cationic porphyrin derivatives,1592

Candida infections – Penetratin and deriva-tives acting as antifungal agents, 212

Candidae – 2–Acylhydrazino–5–arylpyrrolederivatives: Synthesis and antifungal activi-ty evaluation, 1288

Cannabinoid – Synthesis and pharmacologi-cal evaluation of sulfamide–based ana-logues of anandamide, 4889

Cannabinoid receptor – Analogs ofJHU75528, a PET ligand for imaging ofcerebral cannabinoid receptors (CB1):Development of ligands with optimizedlipophilicity and binding affinity, 593

Cannabinoid receptors – Development ofCoMFA and CoMSIA models of affinityand selectivity for indole ligands ofcannabinoid CB1 and CB2 receptors, 2482

Cantagalo virus – Antiviral evaluation ofN–amino–1,2,3–triazoles against Cantagalovirus replication in cell culture, 3777

Capsaicin – Synthesis and antinociceptiveactivity of capsinoid derivatives, 3345

Capsinoid derivatives – Synthesis andantinociceptive activity of capsinoid deriva-tives, 3345

Capsinoid – Synthesis and antinociceptiveactivity of capsinoid derivatives, 3345

Captopril – Captopril and 6–mercaptopurine:Whose SH possesses higher antioxidantability?, 4841

Carbamate – Synthesis and blood glucoselowering effect of novel pyridazinone sub-stituted benzenesulfonylurea derivatives,2673 – Chiral3–(4,5–dihydrooxazol–2–yl)phenyl alkyl-carbamates as novel FAAH inhibitors:Insight into FAAH enantioselectivity bymolecular docking and interaction fields,4179

Carbamides – Synthesis of glycose car-bamides and evaluation of the induction oferythroid differentiation of human ery-throleukemic K562 cells, 745

Carbazolophanes – Synthesis of novel car-bazole based macrocyclic amides as poten-tial antimicrobial agents, 3040

Carbohydrates – Novel pyridazine deriva-tives: Synthesis and antimicrobial activityevaluation, 1989

Carbohydrazide derivatives – Synthesis andantiviral activity of �–carboline derivativesbearing a substituted carbohydrazide at C–3against poliovirus and herpes simplex virus(HSV–1), 4695

Carbonic anhydrase inhibition – A QSARstudy on relationship between structure ofsulfonamides and their carbonic anhydrase

inhibitory activity using the eigenvalue(EVA) method, 3439

Carbonic anhydrase – Synthesis and biolog-ical evaluation of a new family of anti–ben-zylanilinosulfonamides as CA IX inhibitors,511 – Design, synthesis and anticancer eval-uation of novel tetrahydroquinoline deriva-tives containing sulfonamide moiety, 4211

Carbon–11 – Analogs of JHU75528, a PETligand for imaging of cerebral cannabinoidreceptors (CB1): Development of ligandswith optimized lipophilicity and bindingaffinity, 593 – 11C–labelled PIB analoguesas potential tracer agents for in vivo imag-ing of amyloid � in Alzheimer’s disease,1415 – Simple synthesis of carbon–11labeled styryl dyes as new potential PETRNA–specific, living cell imaging probes,2300

Carboranes – Promising carboranylquinazo-lines for boron neutron capture therapy:Synthesis, characterization, and in vitro tox-icity evaluation, 409

Carboxamidine – Synthesis and antiparasiticand antifungal evaluation of 2'–arylsubsti-tuted–1H,1'H–[2,5']bisbenzimidazolyl–5–carboxamidines, 2002

Carboxylic acid amide – Design, synthesisand in vitro antibacterial/antifungal evalua-tion of novel1–ethyl–6–fluoro–1,4–dihy-dro–4–oxo–7(1–piperazinyl)quinoline–3–carboxylicacid derivatives, 4726

Carboxylic acid hydrazides – Synthesis ofnovel pyrazole derivatives and evaluation oftheir antidepressant and anticonvulsantactivities, 3480

Carcinogenic potency database –Development of QSAR models for predict-ing hepatocarcinogenic toxicity of chemi-cals, 3658

Carcinogens – Known drug space as a metricin exploring the boundaries of drug–likechemical space, 5006

Carcinoma cell lines – Synthesis and in vitroantiproliferative activity of novel 1–ben-zhydrylpiperazine derivatives againsthuman cancer cell lines, 1223

Carcinoma cells – Synthesis of2–styrylchromones as a novel class ofantiproliferative agents targeting carcinomacells, 2552

Carcinoma – Antiproliferative activity ofarborescidine alkaloids and derivatives,3810

Cardiotoxicity – Studies on self–aggregationof anthracycline drugs by restrainedmolecular dynamics approach usingnuclear magnetic resonance spectroscopysupported by absorption, fluorescence, dif-fusion ordered spectroscopy and massspectrometry, 1437

Cardiovascular and spasmolytic activities –Synthesis and adrenolytic activity of1–(1H–indol–4–yloxy)–3–(2–(2–methoxyphenoxy)ethylamino)propan–2–ol analogsand its enantiomers. Part 2, 5103

Carotid artery cannulation – Synthesis andpharmacological investigation of 3–(substi-tuted 1–phenylethanone)–4–(substitutedphenyl)–1, 2, 3, 4–tetrahydropyrimi-dine–5–carboxylates, 3645

Page 20: Chal Micro

5150 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Cashew nut shell liquid – Synthesis of benza-mide derivatives of anacardic acid and theircytotoxic activity, 2711

Catalyst – Knowledge based identification ofMAO–B selective inhibitors using pharma-cophore and structure based virtual screen-ing models, 3584 – Pharmacophore model-ing and virtual screening for the discoveryof new transforming growth factor–� type Ireceptor (ALK5) inhibitors, 4259

Catalytic reduction – Novel8–deaza–5,6,7,8–tetrahydroaminopterinderivatives as dihydrofolate inhibitor:Design, synthesis and antifolate activity, 764

Cathepsin G – Natural polyprenylated ben-zophenones inhibiting cysteine and serineproteases, 1230

Cationic cholesterol – Histone deacetylaseinhibitor prodrugs in nanoparticle vectorenhanced gene expression in human cancercells, 4603

Cationic nanoparticle – Histone deacetylaseinhibitor prodrugs in nanoparticle vectorenhanced gene expression in human cancercells, 4603

Cationic peptides – Penetratin and deriva-tives acting as antifungal agents, 212

Cationic peptoids – Synthesis of novelN–protected hydrophobic phenylalaninesand their application in potential antibacte-rials, 1001

Cationic porphyrin – Photodynamic inacti-vation of Candida albicans sensitized bytri– and tetra–cationic porphyrin deriva-tives, 1592

CB1 receptor – Development of CoMFA andCoMSIA models of affinity and selectivityfor indole ligands of cannabinoid CB1 andCB2 receptors, 2482

CB2 receptor – Development of CoMFA andCoMSIA models of affinity and selectivityfor indole ligands of cannabinoid CB1 andCB2 receptors, 2482

CCR5 – Prediction of CCR5 receptor bindingaffinity of substituted 1–(3,3–diphenyl-propyl)–piperidinyl amides and ureas basedon the heuristic method, support vectormachine and projection pursuit regression, 25

CD studies – Circular dichroism studies oftype III collagen mimetic peptides withanti– or pro–aggregant activities on humanplatelets, 2643

CDK – Synthesis of new dipyrrolo– andfuropyrrolopyrazinones related to tripen-tones and their biological evaluation aspotential kinases (CDKs1–5, GSK–3)inhibitors, 708

Cell cycle – Synthesis and biological evalua-tion of novel symmetry bis–enediynes, 35 –5–Benzylidene–hydantoins: Synthesis andantiproliferative activity on A549 lung can-cer cell line, 3471 – Synthesis, cytotoxicityand DNA–binding levels of new type binu-clear platinum(II) complexes, 4772

Cell distribution – Unusual cellular uptake ofcytotoxic 4–hydroxymethyl–3–aminoacri-dine, 4758

Cell proliferation – Synthesis and in vitroantiproliferative activity of novel 1–ben-zhydrylpiperazine derivatives againsthuman cancer cell lines, 1223

Cell protective effect – Facile synthesis and invitro properties of 1–alkyl– and1–alkyl–N–propargyl–1,2,3,4–tetrahydroiso-quinoline derivatives on PC12 cells, 4034

Cell viability – Structure–activity relationshipof seco–tanapartholides isolated fromAchillea falcata for inhibition of HaCaT cellgrowth, 3794

Cell wall – Synthesis and evaluation of invitro anti–tuberculosis activity of N–substi-tuted glycolamides, 289

Cell–cycle arrest – Design, synthesis and pre-liminary biological evaluation ofN–hydroxy–4–(3–phenylpropanamido)ben-zamide (HPPB) derivatives as novel histonedeacetylase inhibitors, 4470

cGMP–dependent protein kinase –Predicting the activity of drugs for a groupof imidazopyridine anticoccidial com-pounds, 4044

Chagas disease – Second generation of2H–benzimidazole 1,3–dioxide derivativesas anti–trypanosomatid agents: Synthesis,biological evaluation, and mode of actionstudies, 4426 – Effect of ruthenium com-plexation on trypanocidal activity of5–nitrofuryl containing thiosemicar-bazones, 4937

Chagas’ disease – In vitro and in vivo antitry-panosomatid activity of 5–nitroindazoles,1034

Chalcone derivatives – Antimalarial pharma-codynamics of chalcone derivatives in com-bination with artemisinin againstPlasmodium falciparum in vitro, 3388

Chalcone – Synthesis of (±)Abyssinone I andrelated compounds: Their anti–oxidant andcytotoxic activities, 2239

Chalcones – Synthesis of chlorovinyl sulfonesas structural analogs of chalcones and theirantiplasmodial activities, 1457 –Substituted quinolinyl chalcones and quino-linyl pyrimidines as a new class ofanti–infective agents, 2081 – Examinationof growth inhibitory properties of syntheticchalcones for which antibacterial activitywas predicted, 2211 – DNA–targetingpyrroloquinoline–linked butenone and chal-cones: Synthesis and biological evaluation,2854 – Anti–oxidant, anti–fungal andanti–leishmanial activities ofn o v e l 3 – [ 4 – ( 1 H – i m i d a z o l – 1 – y l )phenyl]prop–2–en–1–ones, 4654

Characterization – Synthesis, spectral char-acterization, in–vitro microbiological evalu-ation and cytotoxic activities of novelmacrocyclic bis hydrazone, 3552

Charge transfer reaction –Spectrophotometric and HPLC determina-tions of anti–diabetic drugs, rosiglitazonemaleate and metformin hydrochloride, inpure form and in pharmaceutical prepara-tions, 4998

Chemical induced models – Synthesis andanticonvulsant activity of N–(2–hydrox-yethyl) cinnamamide derivatives, 3654

Chemical modification – Chiral gossypolderivatives: Evaluation of their anticanceractivity and molecular modeling, 3961

Chemical nucleases – “Self–activating”chemical nuclease: Ferrocenyl cyclen

Cu(II) complexes act as efficient DNAcleavage reagents in the absence of reduc-tant, 1768

Chemical reactivity – Cytotoxic activity andchemical reactivity of cis–platinum(II) andtrans–palladium(II) complexes with diethyl(pyridinylmethyl)phosphates, 660

Chemiluminescence – Investigation of theantioxidant properties of some new4–hydroxycoumarin derivatives, 3077

Chemometrics – Application of genetic algo-rithm–support vector machine (GA–SVM)for prediction of BK–channels activity, 5023

Chemotaxis – Oligomeric formylpeptideactivity on human neutrophils, 4926

Chiral gossypol – Chiral gossypol deriva-tives: Evaluation of their anticancer activityand molecular modeling, 3961

Chitin biosynthesis – Diacylhydrazine deriv-atives as novel potential chitin biosynthesisinhibitors: Design, synthesis, and struc-ture–activity relationship, 2985

Chitin synthase – Antifungal unsaturatedcyclic Mannich ketones and amino alco-hols: Study of mechanism of action, 1823

Chk1 inhibitors – A three–step synthesisfrom rebeccamycin of an efficient check-point kinase 1 inhibitor, 2234

Chloramine–T – Synthesis of new series of5,6–dihydro–4H–1,2–oxazines via heteroDiels–Alder reaction and evaluation ofantimicrobial activity, 280 – Synthesis andpharmacological evaluation of 1,3,4–oxadi-azole bearing bis(heterocycle) derivativesas anti–inflammatory and analgesic agents,3898

Chloramphenicol – Fluorescence spectroscop-ic investigation of the interaction betweenchloramphenicol and lysozyme, 4083

Chlorovinyl sulfones – Synthesis ofchlorovinyl sulfones as structural analogs ofchalcones and their antiplasmodial activi-ties, 1457

Cholesterol absorption inhibition –2–Azetidinone derivatives: Design, synthe-sis and evaluation of cholesterol absorptioninhibitors, 1638

Cholesterol – Design, synthesis and hypolipi-demic activity of novel 2–(m–tolyloxy)isobutyric acid derivatives, 2679 – Design,synthesis and hypolipidemic activity ofnovel 2–(naphthalen–2–yloxy)propionicacid derivatives as desmethyl fibrateanalogs, 3973

Cholinesterase inhibitor – Design, synthesisand evaluation of galanthamine derivativesas acetylcholinesterase inhibitors, 772

Chromanes – Diversity–oriented synthesis offuro[3,2–f]chromanes with antimycobacter-ial activity, 2497

Chromium peroxide – Blue CrO5 assay: Anovel spectrophotometric method for theevaluation of the antioxidant and oxidantcapacity of various biological substances,4162

Chromone – Synthesis and antitumor activityof novel dithiocarbamate substitutedchromones, 3687

Cinnamamide derivatives – Synthesis andanticonvulsant activity of N–(2–hydrox-yethyl) cinnamamide derivatives, 3654

Page 21: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5151

Circular dichroism – Fluorescence spectro-scopic investigation of the interactionbetween chloramphenicol and lysozyme,4083

Circular dichroism spectra – Inhibitoryeffects of 5–benzylidene barbiturate deriva-tives on mushroom tyrosinase and theirantibacterial activities, 4235

Classification – Classification models forCYP450 3A4 inhibitors and non–inhibitors,2354

Cleavage of DNA – Hydrolytic cleavage ofDNA by urea–bridged macrocyclicpolyamines, 5090

ClHOBT – Synthesis and biochemical evalu-ation of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

Click chemistry – Synthesis and cytotoxicprofile of glycosyl–triazole linked to1,2,4–oxadiazole moiety at C–5 through astraight–chain carbon and oxygen atoms,3571

Clonic convulsions – Synthesis of novelbioactive derivatives of3–(4–chlorophenyl)–2–hydrazino–5,6,7,8–tetrahydrobenzo(b)thieno[2,3–d]pyrimi-dine–4(3H)–ones, 4721

Clotrimazole – Synthesis, Raman, FT–IR,NMR spectroscopic data and antimicrobialactivity of mixed aza–oxo–thia macrocycliccompounds, 365

Clotting assay – Design of novel aminopyrro-lidine factor Xa inhibitors from a screeninghit, 2787

Clubbed triazole–thiazole derivatives –Synthesis of new 4–isopropylthiazolehydrazide analogs and some derivedclubbed triazole, oxadiazole ring systems –A novel class of potential antibacterial, anti-fungal and antitubercular agents, 4739

Cluster analysis – Possible anticancer agents:QSAR analogs of glutamamide: Synthesisand pharmacological activity of1,5–N,N'–disubstituted–2–(substituted ben-zenesulphonyl) glutamamides, 70

C–alkylation – Synthesis and antitubercularscreening of imidazole derivatives, 3350

C–Allyl imidazoles – Synthesis and antituber-cular screening of imidazole derivatives,3350

C–nucleosides – Synthesis and anti–HSV–1evaluation of some pyrazoles and fusedpyrazolopyrimidines, 3285

CNS activity – Synthesis, pharmacologicaland antiviral activity of 1,3–thiazepinederivatives, 4960

CNS depressants activity – Synthesis, anti-convulsant and CNS depressant activity ofsome new bioactive1–(4–substituted–phenyl)–3–(4–oxo–2–phenyl/ethyl–4H–quinazolin–3–yl)–urea, 4335

c–Src – Docking, 3D–QSAR studies and insilico ADME prediction on c–Src tyrosinekinase inhibitors, 990

Co(II) complexes – Synthesis, spectroscopiccharacterization and antibacterial activity ofnew cobalt(II) complexes of unsymmetricaltetradentate (OSN2) Schiff base ligands,4490

Co(II), Zn(II), Cd(II) complexes – Synthesis,characterization and antimicrobial activity

of Co(II), Zn(II) and Cd(II) complexes withN–benzyloxycarbonyl–S–phenylalanine,1537

Combinatorial protocol in multiple linearregression (CP–MLR) – Juglone deriva-tives as antitubercular agents: A rationalefor the activity profile, 2847

Combinatorial Protocol in Multiple LinearRegression (CP–MLR) – Topologicaldescriptors in modeling the agonistic activi-ty of human A3 adenosine receptor ligands:The derivatives of 2–chloro–N6–substitut-ed–4'–thioadenosine–5'–uronamide, 1377

Combretastatin A–4 – A diaryl sulfide, sul-foxide, and sulfone bearing structural simi-larities to combretastatin A–4, 2685

Comet assay – Synthesis and antitumor activ-ity of optically active thiourea and their2–aminobenzothiazole derivatives: A novelclass of anticancer agents, 2923

CoMFA affinity model – Development ofCoMFA and CoMSIA models of affinityand selectivity for indole ligands ofcannabinoid CB1 and CB2 receptors, 2482

CoMFA and CoMSIA models –Development of CoMFA and CoMSIAmodels of cytotoxicity data ofanti–HIV–1–phenylamino–1H–imidazolederivatives, 2400

CoMFA – ‘Sum of activities’ as dependentparameter: A new CoMFA–based approachfor the design of pan PPAR agonists, 42 –Predicting anti–HIV activity of 1,3,4–thia-zolidinone derivatives: 3D–QSARapproach, 1180 – Receptor–based3D–QSAR studies of checkpoint Wee1kinase inhibitors, 1383 – 3D–QSAR studiesof boron–containing dipeptides as protea-some inhibitors with CoMFA and CoMSIAmethods, 1486 – Synthesis, anti–tuberculo-sis activity and 3D–QSAR study of aminoacid conjugates of 4–(adamantan–1–yl)group containing quinolines, 2017 –Thiocarbamates as non–nucleoside HIV–1reverse transcriptase inhibitors:Docking–based CoMFA and CoMSIAanalyses, 2059 – Homology modeling ofMCH1 receptor and validation bydocking/scoring and protein–alignedCoMFA, 2583 – CoMFA and docking stud-ies of 2–phenylindole derivatives with anti-cancer activity, 2822 – 2D– and 3D–QSARstudies on 54 anti–tumor Rubiaceae–typecyclopeptides, 3425 – CoMFA, LeapFrogand blind docking studies on sulfonanilidederivatives acting as selective aromataseexpression regulators, 3445 – Docking and3D–QSAR studies of BMS–806 analogs asHIV–1 gp120 entry inhibitors, 3524 –Application of 3D QSAR CoMFA/CoMSIAand in silico docking studies on novel renininhibitors against cardiovascular diseases,3703 – 3D–QSAR with the aid of pharma-cophore search and docking–based align-ments for farnesyltransferase inhibitors,4070 – Docking–based 3D–QSAR study ofHIV–1 integrase inhibitors, 4276 – 3DQSAR study of the toxicity of trichothecenemycotoxins, 4485

CoMFA selectivity model – Development ofCoMFA and CoMSIA models of affinity

and selectivity for indole ligands ofcannabinoid CB1 and CB2 receptors, 2482

Comparative model – Fragment and knowl-edge–based design of selective GSK–3�inhibitors using virtual screening models,2361

Complex Networks – Multi–target spectralmoments for QSAR and Complex Networksstudy of antibacterial drugs, 4516

Complex networks – Scoring function forDNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Complexes – Synthesis and characterizationof new Pt(II) and Pd(II) complexes with2–quinolinecarboxaldehyde selenosemicar-bazone: Cytotoxic activity evaluation ofCd(II), Zn(II), Ni(II), Pt(II) and Pd(II) com-plexes with heteroaromatic selenosemicar-bazones, 1623 – “Self–activating” chemicalnuclease: Ferrocenyl cyclen Cu(II) com-plexes act as efficient DNA cleavagereagents in the absence of reductant, 1768

Compound action potential – Evaluation ofthe local anaesthetic activity of3–aminobenzo[d]isothiazole derivativesusing the rat sciatic nerve model, 473

Computer–aided design – Design of novelaminopyrrolidine factor Xa inhibitors froma screening hit, 2787

CoMSIA – Predicting anti–HIV activity of1,3,4–thiazolidinone derivatives:3D–QSAR approach, 1180 – 3D–QSARstudies of boron–containing dipeptides asproteasome inhibitors with CoMFA andCoMSIA methods, 1486 – Thiocarbamatesas non–nucleoside HIV–1 reverse transcrip-tase inhibitors: Docking–based CoMFA andCoMSIA analyses, 2059 – Development ofCoMFA and CoMSIA models of affinityand selectivity for indole ligands ofcannabinoid CB1 and CB2 receptors, 2482– 2D– and 3D–QSAR studies on 54anti–tumor Rubiaceae–type cyclopeptides,3425 – Docking and 3D–QSAR studies ofBMS–806 analogs as HIV–1 gp120 entryinhibitors, 3524 – Application of 3D QSARCoMFA/CoMSIA and in silico dockingstudies on novel renin inhibitors against car-diovascular diseases, 3703 – 3D–QSARwith the aid of pharmacophore search anddocking–based alignments for farnesyl-transferase inhibitors, 4070 – NovelBiginelli dihydropyrimidines with potentialanticancer activity: A parallel synthesis andCoMSIA study, 4192 – Docking–based3D–QSAR study of HIV–1 integraseinhibitors, 4276 – 3D QSAR study of thetoxicity of trichothecene mycotoxins, 4485

Condensed pyrimidines – Synthesis, anal-gesic and anti–inflammatory activities eval-uation of some bi–, tri– and tetracyclic con-densed pyrimidines, 4572

Conformation – Synthesis and spectral char-acterization of a new class ofN–(N–methylpiperazinoacetyl)–2,6–diarylpiperidin–4–ones: Antimicrobial, analgesicand antipyretic studies, 577 – 3D–QSARstudies of HDACs inhibitors using pharma-cophore–based alignment, 2868

Page 22: Chal Micro

5152 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Conformational analysis – Penetratin andderivatives acting as antifungal agents, 212

Conformational restriction – Design andsynthesis of calpain inhibitory 6–pyridone2–carboxamide derivatives, 1331

Conformational study – Large ring1,3–bridged 2–azetidinones: Experimentaland theoretical studies, 2071

Conformationally constrained analogues –Conformationally constrained analogues ofN'–(4–tert–butylbenzyl)–N–(4–methylsul-fonylaminobenzyl)thiourea as TRPV1antagonists, 322

Conjugate – Targeting cancer cells withbiotin–dendrimer conjugates, 862 –Synthesis, evaluation and 3D QSAR analy-sis of novel estradiol–RGD octapeptideconjugates with oral anti–osteoporosisactivity, 1689 – Effect of conjugates ofall–trans–retinoic acid and shorter polyenechain analogues with amino acids onprostate cancer cell growth, 3175

Contact–active surface – Contact–activemicrobicidal gold surfaces using immobi-lization of quaternary ammonium thiolderivatives, 4227

Convulsant activity – Prediction of convul-sant activity of gases and vapors, 885

Copper complexes – Synthesis, structure andbiological activity of copper(II) complexesof 4–(2–pyridylmethyl)–1,7–dimethyl–1,4,7–triazonane–2,6–dione and4–(2–pyridylethyl)–1,7–dimethyl–1,4,7–tri-azonane–2,6–dione, 1607

Copper – Copper complexes of pyridinederivatives with superoxide scavenging andantimicrobial activities, 3259

Copper(II) – Metals in anticancer therapy:Copper(II) complexes as inhibitors of the20S proteasome, 4353

Cordycepin – Synthesis and pharmacokineticevaluation of novel N–acyl–cordycepinderivatives with a normal alkyl chain, 665

Corneal permeability – Synthesis, pharma-cological screening, quantum chemical andin vitro permeability studies of N–Mannichbases of benzimidazoles through bovinecornea, 2307

Coumarin – Synthesis and pharmacologicalevaluation of a novel series of 5–(substitut-ed)aryl–3–(3–coumarinyl)–1–phenyl–2–pyrazolines as novel anti–inflammatory andanalgesic agents, 1682 – Synthesis, charac-terization, DNA cleavage and in vitroantimicrobial studies of La(III), Th(IV) andVO(IV) complexes with Schiff bases ofcoumarin derivatives, 2904 –2–Azetidinone derivatives: Design, synthe-sis, in vitro anti–microbial, cytotoxic activi-ties and DNA cleavage study, 5123

Coumarine – Synthesis and antibacterialactivity of some new heterocycles incorpo-rating phthalazine, 4448

Coumarins – Synthesis and evaluation of theantioxidant and anti–inflammatory activityof novel coumarin–3–aminoamides andtheir alpha–lipoic acid adducts, 3020

COX – Adamantane derivatives ofthiazolyl–N–substituted amide, as possiblenon–steroidal anti–inflammatory agents,1198

COX–1 – Synthesis and biological evaluationof 4,5–diphenyloxazolone derivatives onroute towards selective COX–2 inhibitors,1830

COX–1/–2 inhibitors – Design, synthesis andevaluation of tetrahydropyran basedCOX–1/–2 inhibitors, 1278

COX–2 – Design, synthesis and molecularmodeling study of acylated 1,2,4–tria-zole–3–acetates with potential anti–inflam-matory activity, 117 – Synthesis and biolog-ical evaluation of 4,5–diphenyloxazolonederivatives on route towards selectiveCOX–2 inhibitors, 1830

Crinum defixum Ker–Gawl – Anti–genotox-ic hydrazide from Crinum defixum, 2754

Cross–Claisen condensation – Synthesis ofsome novel bioactive 4–oxy/thio substitut-ed–1H–pyrazol–5(4H)–ones via efficientcross–Claisen condensation, 3852

Cryptococcosis – Penetratin and derivativesacting as antifungal agents, 212

Crystal structure – In vitro and in vivo antitu-mor activity of platinum(II) complexes withthiosemicarbazones derived from 2–formyland 2–acetyl pyridine and containing ringincorporated at N(4)–position: Synthesis,spectroscopic study and crystal structure ofplatinum(II) complexes with thiosemicar-bazones, potential anticancer agents, 1296 –Antimicrobial and SOD activities of noveltransition metal ternary complexes of imin-odiacetic acid containing �–diimine as aux-iliary ligand, 2517 – Palladium(II) complex-es with R2edda–derived ligands. Part II.Synthesis, characterization and in vitro anti-tumoral studies of R2eddip esters and palla-dium(II) complexes, 3452 – Synthesis, crys-tal structure, DNA interaction and antioxi-dant activities of two novel water–solubleCu(2�) complexes derivated from2 – o x o – q u i n o l i n e – 3 – c a r b a l d e h y d eSchiff–bases, 4477 – Antitumor and antimy-cobacterial activities of cyclopalladatedcomplexes: X–ray structure of[ P d ( C 2 , N – d m b a ) ( B r ) ( t u ) ](dmba=N ,N–d ime thy lbenzy lamine ,tu=thiourea), 4611

Crystallographic study – Synthesis andantiproliferative activity of3–amino–N–phenyl–1H–indazole–1–car-boxamides, 165

CT–DNA – Synthesis and characterization ofdinuclear macrocyclic cobalt(II), copper(II)and zinc(II) complexes derived from2,2,2',2'–S,S[bis(bis–N,N–2–thiobenzimida-zolyloxalato–1,2–ethane)]: DNA bindingand cleavage studies, 834 – Synthesis,Raman, FT–IR, NMR spectroscopic charac-terization, antimicrobial activity, cytotoxici-ty and DNA binding of new mixedaza–oxo–thia macrocyclic compounds,4681

Cu(II) complex – Synthesis and characteriza-tion of the Zn(II) and Cu(II) piperidinylisoeuxanthone complexes: DNA–bindingand cytotoxic activity, 4509

Cu(II) complexes – Copper(II) anduranyl(II) complexes with acylthiosemi-carbazide: Synthesis, characterization,antibacterial activity and effects on the

growth of promyelocytic leukemia cellsHL–60, 3323

Curcumin analogue – Synthesis, crystalstructure and anti–inflammatory propertiesof curcumin analogues, 915

Curtius rearrangement – Synthesis of newdipyrrolo– and furopyrrolopyrazinonesrelated to tripentones and their biologicalevaluation as potential kinases (CDKs1–5,GSK–3) inhibitors, 708

CXCR3 – A novel QSAR model for predict-ing the inhibition of CXCR3 receptor by4–N–aryl–[1,4] diazepane ureas, 877

CXCR4 antagonists – Bis–14–memberedring diketal diamines: Synthesis and evalu-ation of their anti–HIV and anti–tumoralactivities, 3138

Cyanine – An in vitro characterization studyof new near infrared dyes for molecularimaging, 3496

Cyanoacetamide – Synthesis and anti–tumoractivities of some new pyridines and pyra-zolo[1,5–a]pyrimidines, 3519

Cyanothioacetamide – Synthesis andanti–tumor activities of some new pyridinesand pyrazolo[1,5–a]pyrimidines, 3519

Cyclen – “Self–activating” chemical nuclease:Ferrocenyl cyclen Cu(II) complexes act asefficient DNA cleavage reagents in theabsence of reductant, 1768

Cyclic phosphoramidate – Cyclic phospho-ramidates as prodrugs of 2'–C–methylcyti-dine, 3765

Cyclic voltammetry – Comparative study ofthe trypanocidal activity of the methyl1–nitrophenyl–1,2,3,4–9H–tetrahydro–�–carboline–3–carboxylate derivatives andbenznidazole using theoretical calculationsand cyclic voltammetry, 1745 – Synthesis,characterization, DNA cleavage and in vitroantimicrobial studies of La(III), Th(IV) andVO(IV) complexes with Schiff bases ofcoumarin derivatives, 2904

Cyclic–imide – Novel cyclic–imide pep-tidomimetics as aminopeptidase Ninhibitors. Design, chemistry and activityevaluation. Part I, 4819

Cyclin–dependent kinase – Synthesis of newdipyrrolo– and furopyrrolopyrazinonesrelated to tripentones and their biologicalevaluation as potential kinases (CDKs1–5,GSK–3) inhibitors, 708

Cyclization – Synthesis and biological evalu-ation of 3,6–disubstituted [1,2,4]triazo-lo[3,4–b][1,3,4]thiadiazole derivatives as anovel class of potential anti–tumor agents,2776

Cycloaddition – Regioselective synthesis andantimicrobial screening of novel ketocar-bazolodispiropyrrolidine derivatives, 959 –Synthesis and antimicrobial activity of new1–alkyl/cyclohexyl–3,3–diaryl–1'–methyl-spiro[azetidine–2,3'–indoline]–2',4–diones,2265

Cyclodehydration – Synthesis and structureanalysis of cyclodehydration product ofpiroxicam: A metabolite detected in dogsand monkeys, 3368

Cyclohexanocoumarins – Synthesis andanti–inflammatory evaluation of novelangularly or linearly fused coumarins, 5012

Page 23: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5153

Cyclohexanone – Synthesis, crystal structureand anti–inflammatory properties of cur-cumin analogues, 915

Cyclolinopeptide A – Synthesis and immuno-suppressive activity of cyclolinopeptide Aanalogues containing homophenylalanine,3731

Cyclooxygenase inhibition – Synthesis andbiological evaluation of 4,5–diphenyloxa-zolone derivatives on route towards selec-tive COX–2 inhibitors, 1830

Cyclooxygenases – Design, synthesis andevaluation of tetrahydropyran basedCOX–1/–2 inhibitors, 1278

Cyclopalladated complex – Antitumor andantimycobacterial activities of cyclopalla-dated complexes: X–ray structure of[ P d ( C 2 , N – d m b a ) ( B r ) ( t u ) ](dmba=N ,N–d ime thy lbenzy lamine ,tu=thiourea), 4611

Cyclopentane derivatives – New cyclopen-tane derivatives as inhibitors of steroidmetabolizing enzymes AKR1C1 andAKR1C3, 2563

Cyclopentanocoumarins – Synthesis andanti–inflammatory evaluation of novelangularly or linearly fused coumarins, 5012

Cyclopeptide – Synthesis and biochemicalevaluation of a cyclic RGD oxorheniumcomplex as new ligand of �V�3 integrin,3394

Cyclopropanecarboxamide – Synthesis, anti-fungal activities and 3D–QSAR study ofN–(5–substituted–1,3,4–thiadiazol–2–yl)cyclopropanecarboxamides, 2782

Cyclopropanespirohydantoin – Synthesisand potential anticonvulsant activity of newN–3–substituted 5,5–cyclopropanespirohy-dantoins, 296

Cycloxygenase–2 – New pyridone, thioxopy-ridine, pyrazolopyridine and pyridine deriv-atives that modulate inflammatory media-tors in stimulated RAW 264.7 murinemacrophage, 4547

CYP11B1 – Novel CYP17 inhibitors:Synthesis, biological evaluation,structure–activity relationships and model-ling of methoxy– and hydroxy–substitutedmethyleneimidazolyl biphenyls, 2765

CYP3A4 – Novel CYP17 inhibitors:Synthesis, biological evaluation,structure–activity relationships and model-ling of methoxy– and hydroxy–substitutedmethyleneimidazolyl biphenyls, 2765

CYP51 – Design, synthesis, and biologicalevaluation of novel triazole derivatives asinhibitors of cytochrome P45014�–demethylase, 1913

Cysticidal activity – Synthesis and in vitrocysticidal activity of new benzimidazolederivatives, 1794

Cytochrome 3A4 – Comparative chemomet-ric modeling of cytochrome 3A4 inhibitoryactivity of structurally diverse compoundsusing stepwise MLR, FA–MLR, PLS, GFA,G/PLS and ANN techniques, 2913

Cytochrome P450 3A4 – Classification mod-els for CYP450 3A4 inhibitors andnon–inhibitors, 2354

Cytochrome P450 enzymes – ExploringQSAR and QAAR for inhibitors of

cytochrome P450 2A6 and 2A5 enzymesusing GFA and G/PLS techniques, 1941

Cytochrome P450 protein – The metabolismof CYP2C9 and CYP2C19 for gliclazide byhomology modeling and docking study, 854

Cytoprotection – Synthesis and antioxidantpotential of novel synthetic benzophenoneanalogues, 2724

Cytostatic activity – The novel phosphorami-date derivatives of NSAID 3–hydrox-ypropylamides: Synthesis, cytostatic andantiviral activity evaluations, 143

Cytotoxic activities – Synthesis and in vitrocytotoxic evaluation of novel3,4,5–trimethoxyphenyl substituted �–car-boline derivatives, 533

Cytotoxic activity – Cyclocondensation reac-tion of heterocyclic carbonyl compounds,Part XIII: Synthesis and cytotoxic activityof some3,7–diaryl–5–(3,4,5–trimethoxyphenyl)pyrazolo[4,3–e][1,2,4]triazines, 891 –(±)–3,4–Dihydroxy–8,9–methylene-dioxypterocarpan and derivatives:Cytotoxic effect on human leukemia celllines, 920 – 2–Acylhydrazino–5–arylpyr-role derivatives: Synthesis and antifungalactivity evaluation, 1288 – Synthesis,antimicrobial and cytotoxic activities ofsome 5–arylidene–4–thioxo–thiazoli-dine–2–ones, 2038 – Synthesis and bioassayof a new class of heterocycles pyrrolyl oxa-diazoles/thiadiazoles/triazoles, 2313 –Synthesis, characterisation and in vitrocytotoxicity studies of a series of chiral plat-inum(II) complexes based on the2–aminomethylpyrrolidine ligand: X–raycrystal structure of [PtCl2(R–dimepyrr)](R–dimepyrr=N–dimethyl–2(R)–aminomethylpyrrolidine), 2807 – Novel topoiso-merase I–targeting antitumor agents synthe-sized from the N,N,N–trimethylammoniumderivative of ARC–111,5H–2,3–dimethoxy–8,9–methylene-dioxy–5–[(2–N,N,N–trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin–6–oneiodide, 3433 – Synthesis and cytotoxic pro-file of glycosyl–triazole linked to1,2,4–oxadiazole moiety at C–5 through astraight–chain carbon and oxygen atoms,3571 – Antiproliferative activity ofarborescidine alkaloids and derivatives,3810 – Synthesis and characterization of theZn(II) and Cu(II) piperidinyl isoeuxanthonecomplexes: DNA–binding and cytotoxicactivity, 4509 – Dialkylamino and nitrogenheterocyclic analogues of hexadecylphos-phocholine and cetyltrimetylammoniumbromide: Effect of phosphate group andenvironment of the ammonium cation ontheir biological activity, 4970

Cytotoxic effect – Cytotoxic and genotoxiceffects of [Ru(phi)3]2� evaluated byAmes/Salmonella and MTT methods, 2601

Cytotoxic – Discovery of a new family ofbis–8–hydroxyquinoline substituted benzy-lamines with pro–apoptotic activity in can-cer cells: Synthesis, structure–activity rela-tionship, and action mechanism studies, 558– Cytotoxic, antioxidant activities and struc-ture activity relationship of some newly

synthesized terpenoidal oxaliplatin analogs,901 – Synthesis and in vitro cytotoxicity of9–anilinoacridines bearing N–mustardresidue on both anilino and acridine rings,3056 – Synthesis of new acridines andhydrazones derived from cyclic �–diketonefor cytotoxic and antiviral evaluation, 3680– Synthesis, Raman, FT–IR, NMR spectro-scopic characterization, antimicrobial activ-ity, cytotoxicity and DNA binding of newmixed aza–oxo–thia macrocyclic com-pounds, 4681

Cytotoxic properties – Synthesis and biolog-ical evaluation of cytotoxic properties ofstilbene–based resveratrol analogs, 701

Cytotoxic, human cervical cancer (HeLa)cells – 2,3–Disubstituted–1,4–naphtho-quinones, 12H–benzo[b]phenoth-iazine–6,11–diones and related compounds:Synthesis and Biological evaluation aspotential antiproliferative and antifungalagents, 1086

Cytotoxicity assays – Antitumor and antimy-cobacterial activities of cyclopalladatedcomplexes: X–ray structure of[ P d ( C 2 , N – d m b a ) ( B r ) ( t u ) ](dmba=N ,N–d ime thy lbenzy lamine ,tu=thiourea), 4611

Cytotoxicity data – Development of CoMFAand CoMSIA models of cytotoxicity data ofanti–HIV–1–phenylamino–1H–imidazolederivatives, 2400

Cytotoxicity – The cytotoxic properties andpreferential toxicity to tumour cells dis-played by some2,4–bis(benzylidene)–8–methyl–8–azabicy-clo[3.2.1] octan–3–ones and 3,5–bis(ben-zylidene)–1–methyl–4–piperidones, 54 –Synthesis, cytotoxicity and effects of some1,2,4–triazole and 1,3,4–thiadiazole deriva-tives on immunocompetent cells, 63 –Synthesis, cytotoxicity and apoptosis ofnaphthalimide polyamine conjugates asantitumor agents, 393 – Design, synthesisand biological evaluation of novel fluorinat-ed docetaxel analogues, 482 – Cytotoxicactivity and chemical reactivity of cis–plat-inum(II) and trans–palladium(II) complex-es with diethyl (pyridinylmethyl)phos-phates, 660 – Synthetic, structural and bio-chemical studies of polynuclearplatinum(II) complexes with heterocyclicligands, 1041 – Cytotoxicity and TOP1–tar-geting activity of 8– and 9–amino deriva-tives of 5–butyl– and 5–(2–N,N–dimethy-lamino)ethyl–5H–dibenzo[c,h][1,6]naph-thyridin–6–ones, 1471 – Gallium(III) com-plexes of 2–pyridineformamide thiosemi-carbazones: Cytotoxic activity againstmalignant glioblastoma, 1870 – Synthesis,antimicrobial and cytotoxic activities of1,3,4–oxadiazoles, 1,3,4–thiadiazoles and1,2,4–triazoles, 2106 – Synthesis, character-ization and antitumor activity of new typebinuclear platinum(II) complexes, 2322 –Synthesis and biological evaluation of abi-etic acid derivatives, 2468 – A diaryl sul-fide, sulfoxide, and sulfone bearing struc-tural similarities to combretastatin A–4,2685 – Synthesis, characterization and cyto-toxicity of ammine/ethylamine platinum(II)

Page 24: Chal Micro

5154 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

complexes with carboxylates, 2758 – Todetermine the cytotoxicity of chlorambuciland one of its nitro–derivatives, conjugatedto prasterone and pregnenolone, towardseight human cancer cell–lines, 2944 –Synthesis and in vitro antitumor activities ofnovel 4–anilinoquinazoline derivatives,3046 – An in vitro characterization study ofnew near infrared dyes for molecular imag-ing, 3496 – Synthesis and cytotoxic activityof �–santonin derivatives, 3739 – Naturaltanshinone–like heterocyclic–fusedortho–quinones from regioselectiveDiels–Alder reaction: Synthesis and cyto-toxicity evaluation, 3915 – Novel modifiedsteroid derivatives of androstanolone aschemotherapeutic anti–cancer agents, 3936– Chiral gossypol derivatives: Evaluation oftheir anticancer activity and molecular mod-eling, 3961 – Facile synthesis and in vitroproperties of 1–alkyl– and1–alkyl–N–propargyl–1,2,3,4–tetrahy-droisoquinoline derivatives on PC12 cells,4034 – Novel 3,3'–diindolylmethane deriva-tives: Synthesis and cytotoxicity, structuralcharacterization in solid state, 4136 –Design and one–pot synthesis of�–aminophosphonates andbis(�–aminophosphonates) by iron(III)chloride and cytotoxic activity, 4266 –Novel naphthalimide derivatives as poten-tial apoptosis–inducing agents: Design, syn-thesis and biological evaluation, 4674 –Synthesis of new 4–isopropylthiazolehydrazide analogs and some derivedclubbed triazole, oxadiazole ring systems –A novel class of potential antibacterial, anti-fungal and antitubercular agents, 4739 –Synthesis, cytotoxicity and DNA–bindinglevels of new type binuclear platinum(II)complexes, 4772 – Cytotoxicity and effectsof 1,10–phenanthroline and5–amino–1,10–phenanthroline derivativeson some immunocompetent cells, 5099 –2–Azetidinone derivatives: Design, synthe-sis, in vitro anti–microbial, cytotoxic activi-ties and DNA cleavage study, 5123

Cytotoxicity, antiviral activity Thioureaand 1,3–thiazepine derivatives of tricyclicimide – Synthesis, pharmacological andantiviral activity of 1,3–thiazepine deriva-tives, 4960

Cytotoxicy – Synthesis of benzamide deriva-tives of anacardic acid and their cytotoxicactivity, 2711

Cytotoxity – Synthesis and immunosuppres-sive activity of cyclolinopeptide A ana-logues containing homophenylalanine,3731

DDAPYs – QSAR studies for diarylpyrimidines

against HIV–1 reverse transcriptasewild–type and mutant strains, 625

DBA/2 mice – Solution–phase parallel synthe-sis and evaluation of anticonvulsant activityof N–substituted–3,4–dihydroisoquino-line–2(1H)–carboxamides, 1349

DCC – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

DCM – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

Dendrimer – Targeting cancer cells withbiotin–dendrimer conjugates, 862 –Generation–dependent encapsulation/elec-trostatic attachment of phenobarbital mole-cules by poly(amidoamine) dendrimers:Evidence from 2D–NOESY investigations,2219

Dendritic Jeffamines – Synthesis, characteri-zation and antimicrobial activity of watersoluble dendritic macromolecules, 1093

Density functional theory – Computationalstudy of the electronic structure characteri-zation of a novelanti–inflammatory tripep-tide derived from monocyte locomotioninhibitoryfactor (MLIF)–pentapeptide, 3114

Deoxybenzoin derivatives – Amines andoximes derived from deoxybenzoins asHelicobacter pylori urease inhibitors, 2246

Depression – Novel4–aryl–pyrido[1,2–c]pyrimidines with dualSSRI and 5–HT1A activity, Part 1, 1710

Depside – Synthesis, characterization andstructure–activity relationship analysis ofnovel depsides as potential antibacterials,1779

Derivative reagent – A novel spectrophoto-metric method for the determination ofaminophylline with boric acid in pharma-ceutical and mixed serum samples, 1452

Derivative spectrophotometry –Spectrophotometric and HPLC determina-tions of anti–diabetic drugs, rosiglitazonemaleate and metformin hydrochloride, inpure form and in pharmaceutical prepara-tions, 4998

Designed multiple ligands – ‘Sum of activi-ties’ as dependent parameter: A newCoMFA–based approach for the design ofpan PPAR agonists, 42

Desirability – Application ofdesirability–based multi(bi)–objective opti-mization in the design of selectivearylpiperazine derivates for the 5–HT1Aserotonin receptor, 5045

Desmethylfibrates – Design, synthesis andhypolipidemic activity of novel 2–(naph-thalen–2–yloxy)propionic acid derivativesas desmethyl fibrate analogs, 3973

Detoxification – Sulphonamide–basedbombesin prodrug analogues for glutathionetransferase, useful in targeted cancerchemotherapy, 2009

DFP – Synthesis and evaluation of novelbis–pyridinium oximes as reactivators ofDFP–inhibited acetylcholinesterase, 1335

DFT calculations – The structure ofRimonabant in the solid state and in solu-tion: An experimental and theoretical study,1864 – Palladium(II) complexes withR2edda–derived ligands. Part II. Synthesis,characterization and in vitro antitumoralstudies of R2eddip esters and palladium(II)complexes, 3452

DFT – Molecular modeling and inhibition ofphospholipase A2 by polyhydroxy phenoliccompounds, 312 – A theoretical antioxidantpharmacophore for resveratrol, 1644 –Novel trans–dichloridoplatinum(II) com-

plexes with 3– and 4–acetylpyridine:Synthesis, characterization, DFT calcula-tions and cytotoxicity, 1921 – A QSARstudy on relationship between structure ofsulfonamides and their carbonic anhydraseinhibitory activity using the eigenvalue(EVA) method, 3439

Di(hetero)arylamines – QSAR model forpredicting radical scavenging activity ofdi(hetero)arylamines derivatives ofbenzo[b]thiophenes, 1952

Diabetes – Discovery of novel acetanilidederivatives as potent and selective�3–adrenergic receptor agonists, 2533 –Stimulatory effect of apigenin–6–C–�–l–fucopyranoside on insulin secretion andglycogen synthesis, 4668

Diacylhydrazine – Diacylhydrazine deriva-tives as novel potential chitin biosynthesisinhibitors: Design, synthesis, and struc-ture–activity relationship, 2985

Diagnosis – 11C–labelled PIB analogues aspotential tracer agents for in vivo imagingof amyloid � in Alzheimer’s disease, 1415

Diamidines – Synthesis and antiprotozoalactivities of dicationicbis(phenoxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Diamine H3 antagonists – Diamine–basedhuman histamine H3 receptor antagonists:(4–Aminobutyn–1–yl)benzylamines, 4098

Diamine – Design, synthesis, structure–activ-ity relationship and antibacterial activityseries of novel imidazo fused quinolone car-boxamides, 1570

Diaminopyrazoles – Synthesis, antimicrobialand antioxidant activities of substitutedpyrazoles, isoxazoles, pyrimidine and thiox-opyrimidine derivatives, 4557

Diaminopyrimidines – Synthesis, antimicro-bial and antioxidant activities of substitutedpyrazoles, isoxazoles, pyrimidine and thiox-opyrimidine derivatives, 4557

Diaminothioxopyrimidines – Synthesis,antimicrobial and antioxidant activities ofsubstituted pyrazoles, isoxazoles, pyrimi-dine and thioxopyrimidine derivatives,4557

Diaryl sulfide – A diaryl sulfide, sulfoxide,and sulfone bearing structural similarities tocombretastatin A–4, 2685

Diaryl sulfone – A diaryl sulfide, sulfoxide,and sulfone bearing structural similarities tocombretastatin A–4, 2685

Diaryl sulfoxide – A diaryl sulfide, sulfoxide,and sulfone bearing structural similarities tocombretastatin A–4, 2685

Diarylketenes – Synthesis and antimicrobialactivity of new1–alkyl/cyclohexyl–3,3–diaryl–1'–methyl-spiro[azetidine–2,3'–indoline]–2',4–diones,2265

Diarylpentanoids – Synthesis and biologicalevaluation of curcumin–like diarylpen-tanoid analogues for anti–inflammatory,antioxidant and anti–tyrosinase activities,3195

Diazine salts – Diazinium salts with dihy-droxyacetophenone skeleton: Syntheses andantimicrobial activity, 2275

Page 25: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5155

Diazo chemistry – Application of phosphonylcarbanions to highly regioselective synthe-sis of some diazaphospholes and pyra-zolinyl phosphonates, 526

Diazo compounds – Antiviral evaluation ofN–amino–1,2,3–triazoles against Cantagalovirus replication in cell culture, 3777

Dibenzobarrelene – Synthesis and antibacter-ial activity of some new thiazole and thio-phene derivatives, 4434

Diclofenac sodium – Synthesis, analgesic andanti–inflammatory activities of novel3–(4–acetamido–benzyl)–5–substitut-ed–1,2,4–oxadiazoles, 794

Dideoxy fluoro ketonucleosides – Dideoxyfluoro–ketopyranosyl nucleosides as potentantiviral agents: Synthesis and biologicalevaluation of 2,3– and 3,4–dideoxy–3–fluo-ro–4– and –2–keto–�–d–glucopyranosylderivatives of N4–benzoyl cytosine, 2696

Diels–Alder reaction – Naturaltanshinone–like heterocyclic–fusedortho–quinones from regioselectiveDiels–Alder reaction: Synthesis and cyto-toxicity evaluation, 3915

Diffusion ordered spectroscopy – Studies onself–aggregation of anthracycline drugs byrestrained molecular dynamics approachusing nuclear magnetic resonance spec-troscopy supported by absorption, fluores-cence, diffusion ordered spectroscopy andmass spectrometry, 1437

Difluorobenzimidazole – SAR study ofclubbed [1,2,4]–triazolyl with fluorobenz-imidazoles as antimicrobial and antituber-culosis agents, 2930

Dihydrazones – Novel pyridazine derivatives:Synthesis and antimicrobial activity evalua-tion, 1989

Diltiazem – Mechanistic aspects of benzoth-iazepines: A class of antiarrhythmic drugs, 1

Dimedone – Microwave–induced synthesisand anti–microbial activities of7,10,11,12–tetrahydrobenzo[c]acridin–8(9H)–one derivatives, 976

Dioxazole – New derivatives of 3,5–substitut-ed–1,4,2–dioxazoles: Synthesis and activityagainst Entamoeba histolytica, 926

Dioxime – Synthesis, characterization, anti-amoebic activity and toxicity of novel bis-dioxazole derivatives, 4747

Dioxolocoumarins – Synthesis andanti–inflammatory evaluation of novelangularly or linearly fused coumarins, 5012

DIPEA – Synthesis and biochemical evalua-tion of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

Dipeptide boronate – 3D–QSAR studies ofboron–containing dipeptides as proteasomeinhibitors with CoMFA and CoMSIA meth-ods, 1486

Dipeptide – Structure–activity relationshipsfor dipeptide prodrugs of acyclovir:Implications for prodrug design, 2339

Dipeptidyl peptidase IV inhibitors –Synthesis and evaluation of structurallyconstrained imidazolidin derivatives aspotent dipeptidyl peptidase IV inhibitors,3318

Dipeptidyl peptidase IV – Synthesis and use of4–peptidylhydrazido–N–hexyl–1,8–naph-

thalimides as fluorogenic histochemical sub-strates for dipeptidyl peptidase IV and tripep-tidyl peptidase I, 384

Diphenylmaleimide derivate – Discovering anew analogue of thalidomide which may beused as a potent modulator of TNF–� pro-duction, 3533

Dipyrrolopyrazinone – Synthesis of newdipyrrolo– and furopyrrolopyrazinonesrelated to tripentones and their biologicalevaluation as potential kinases (CDKs1–5,GSK–3) inhibitors, 708

Disk diffusion – Synthesis, Raman, FT–IR,NMR spectroscopic data and antimicrobialactivity of mixed aza–oxo–thia macrocycliccompounds, 365

D i s p i r o [ 1 H – i n d e n e – 2 , 3 ' – p y r r o l i -dine–2',3"–[3H]indole]–1,2"(1"H)–dione –Regioselective synthesis ofdispiro[1H–indene–2,3'–pyrrolidine–2',3"–[3H]indole]–1,2"(1"H)–diones of potentialanti–tumor properties, 91

D i s p i r o [ 3 H – i n d o l e – 3 , 2 ' – p y r r o l i -dine–3',3"–piperidine]–2(1H),4"–diones– Regioselective synthesis and stereochem-ical structure of anti–tumor activedispiro[3H–indole–3,2'–pyrrolidine–3',3"–piperidine]–2(1H),4"–diones, 1257

Dispiropyrrolidine – Regioselective synthe-sis and antimicrobial screening of novelketocarbazolodispiropyrrolidine deriva-tives, 959

Dithiazoles – Mechanism of unusual forma-tion of 3–(5–phenyl–3H–[1,2,4]dithia-zol–3–yl)chromen–4–ones and4–oxo–4H–chromene–3–carbothioic acidN–phenylamides and their antimicrobialevaluation, 3209

Dithiocarbamate – Synthesis and antitumoractivity of novel dithiocarbamate substitut-ed chromones, 3687

DNA binding – Synthesis of novelbenzo[h]quinolines: Wound healing, anti-bacterial, DNA binding and in vitro antiox-idant activity, 981 – DNA binding andantimicrobial studies of polymer–copper(II)complexes containing 1,10–phenanthrolineand l–phenylalanine ligands, 1878 –Synthesis, crystal structure, antioxidantactivities and DNA–binding studies of theLn(III) complexes with 7–methoxy-chromone–3–carbaldehyde–(4'–hydroxy)benzoyl hydrazone, 2425 – Synthesis, crys-tal structure, DNA interaction and antioxi-dant activities of two novel water–solubleCu(2�) complexes derivated from2 – o x o – q u i n o l i n e – 3 – c a r b a l d e h y d eSchiff–bases, 4477

DNA binding studies – Synthesis, characteri-zation, DNA binding properties and antioxi-dant activity of Ln(III) complexes with hes-peretin–4–one–(benzoyl) hydrazone, 4585

DNA cleavage – “Self–activating” chemicalnuclease: Ferrocenyl cyclen Cu(II) com-plexes act as efficient DNA cleavagereagents in the absence of reductant, 1768 –2–Azetidinone derivatives: Design, synthe-sis, in vitro anti–microbial, cytotoxic activi-ties and DNA cleavage study, 5123

DNA damage – Synthesis and antitumoractivity of optically active thiourea and their

2–aminobenzothiazole derivatives: A novelclass of anticancer agents, 2923

DNA interaction – Synthesis and affinity toDNA of phenylbenzoimidazoles and ben-zoimidazo[1,2–c]quinazolines, 3305 –Synthesis, spectroscopic characterization,X–ray structure and evaluation of bindingparameters of new triorganotin(IV) dithio-carboxylates with DNA, 3986

DNA intercalation – Photochemical electro-cyclisation of 3–vinylindoles to pyri-do[2,3–a]–, pyrido[4,3–a]– andthieno[2,3–a]–carbazoles: Design, synthe-sis, DNA binding and antitumor cell cyto-toxicity, 3235

DNA ligands – Photochemical electrocyclisa-tion of 3–vinylindoles to pyrido[2,3–a]–,pyrido[4,3–a]– and thieno[2,3–a]–car-bazoles: Design, synthesis, DNA bindingand antitumor cell cytotoxicity, 3235

DNA minor groove binding – Photochemicalelectrocyclisation of 3–vinylindoles to pyri-do[2,3–a]–, pyrido[4,3–a]– andthieno[2,3–a]–carbazoles: Design, synthe-sis, DNA binding and antitumor cell cyto-toxicity, 3235

DNA – Synthesis and DNA–binding studies oftwo ruthenium(II) complexes of an interca-lating ligand, 2044 – Synthesis, characteri-zation, DNA cleavage and in vitro antimi-crobial studies of La(III), Th(IV) andVO(IV) complexes with Schiff bases ofcoumarin derivatives, 2904 – Hydrolyticcleavage of DNA by urea–bridged macro-cyclic polyamines, 5090

DNA–alkylating agents – Synthesis and invitro cytotoxicity of 9–anilinoacridinesbearing N–mustard residue on both anilinoand acridine rings, 3056

DNA–binding – Synthesis and characteriza-tion of the Zn(II) and Cu(II) piperidinylisoeuxanthone complexes: DNA–bindingand cytotoxic activity, 4509 – Synthesis,cytotoxicity and DNA–binding levels ofnew type binuclear platinum(II) complexes,4772

DNA–drug docking – Scoring function forDNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

d–Glucopyranosyl – Synthesis of substitut-ed–phenyl–1,2,4–triazol–3–thione ana-logues with modified d–glucopyranosylresidues and their antiproliferative activi-ties, 4716

d–Phenylalanine – Colon–specific mutualamide prodrugs of 4–aminosalicylic acid fortheir mitigating effect on experimental coli-tis in rats, 131

DOCA–salt hypertension – Synthesis andpharmacological investigation of 3–(substi-tuted 1–phenylethanone)–4–(substitutedphenyl)–1, 2, 3, 4–tetrahydropyrimi-dine–5–carboxylates, 3645

Docetaxel – Design, synthesis and biologicalevaluation of novel fluorinated docetaxelanalogues, 482

Docking – ‘Sum of activities’ as dependentparameter: A new CoMFA–based approachfor the design of pan PPAR agonists, 42 –

Page 26: Chal Micro

5156 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Design, synthesis and molecular modelingstudy of acylated 1,2,4–triazole–3–acetateswith potential anti–inflammatory activity,117 – Synthesis, antitubercular activity anddocking study of novel cyclic azole substi-tuted diphenyl ether derivatives, 492 –Docking, 3D–QSAR studies and in silicoADME prediction on c–Src tyrosine kinaseinhibitors, 990 – Structure–based virtualscreening for identification of novel11�–HSD1 inhibitors, 1167 – Synthesis andbiological evaluation of 4,5–diphenyloxa-zolone derivatives on route towards selec-tive COX–2 inhibitors, 1830 – Fragmentand knowledge–based design of selectiveGSK–3� inhibitors using virtual screeningmodels, 2361 – Synthesis, pharmacologicaland in silico evaluation of1–(4–di–hydroxy–3,5–dioxa–4–borabicy-clo[4.4.0]deca–7,9,11–trien–9–yl)–2–(tert–butylamino)ethanol, a compound designedto act as a �2 adrenoceptor agonist, 2840 –Important pharmacophoric features of panPPAR agonists: Common chemical featureanalysis and virtual screening, 3488 –Docking and 3D–QSAR studies ofBMS–806 analogs as HIV–1 gp120 entryinhibitors, 3524 – Knowledge based identi-fication of MAO–B selective inhibitorsusing pharmacophore and structure basedvirtual screening models, 3584 – Discoveryof potential new InhA direct inhibitorsbased on pharmacophoreand 3D–QSARanalysis followed by in silico screening,3718 – Active site directed docking studies:Synthesis and pharmacological evaluationof cis–2,6–dimethyl piperidine sulfon-amides as inhibitors of acetylcholinesterase,4057 – NovelN–(3–carboxyl–9–benzyl–�–carboline–1–yl)ethylamino acids: Synthesis, anti–tumorevaluation, intercalating determination, 3DQSAR analysis and docking investigation,4153 – Design and one–pot synthesis of�–aminophosphonates andbis(�–aminophosphonates) by iron(III)chloride and cytotoxic activity, 4266 –Docking–based 3D–QSAR study of HIV–1integrase inhibitors, 4276 – Design, synthe-sis and pharmacological screening of novelnitric oxide donors containing1,5–diarylpyrazolin–3–one as nontoxicNSAIDs, 4622 – Discovery of potentialZAP–70 kinase inhibitors: Pharmacophoredesign, database screening and dockingstudies, 4793

Docking study – CoMFA and docking studiesof 2–phenylindole derivatives with anti-cancer activity, 2822

Docking/scoring – Homology modeling ofMCH1 receptor and validation bydocking/scoring and protein–alignedCoMFA, 2583

Dopamine receptors – Structure–activityrelationship of dopaminergic halogenated1–benzyl–tetrahydroisoquinoline deriva-tives, 4616

Dopamine uptake – Structure–activity rela-tionship of dopaminergic halogenated1–benzyl–tetrahydroisoquinoline deriva-tives, 4616

Double emulsion – An investigation into therole of surfactants in controlling particlesize of polymeric nanocapsules containingpenicillin–G in double emulsion, 2392

Doxorubicin – Total synthesis and anticanceractivity of highly potent novel glycolipidderivatives, 3120

DPPH radical scavenging activity – A facilesynthesis of novel biologically active4–hydroxy–N'–(benzylidene)–2H–benzo[e][1,2]thiazine–3–carbohydrazide 1,1–diox-ides, 1311

Drug candidates – Synthesis and characteri-zation of dinuclear macrocyclic cobalt(II),copper(II) and zinc(II) complexes derivedfrom 2,2,2',2'–S,S[bis(bis–N,N–2–thiobenz-imidazolyloxalato–1,2–ethane)]: DNAbinding and cleavage studies, 834

Drug chemical space – Investigation of theincidence of “undesirable” molecular moi-eties for high–throughput screening com-pound libraries in marketed drug com-pounds, 1128

Drug delivery – Generation–dependentencapsulation/electrostatic attachment ofphenobarbital molecules by poly(ami-doamine) dendrimers: Evidence from2D–NOESY investigations, 2219 –Structure–activity relationships for dipep-tide prodrugs of acyclovir: Implications forprodrug design, 2339

Drug design – 3D–QSAR studies ofboron–containing dipeptides as protea-some inhibitors with CoMFA andCoMSIA methods, 1486 – Scoring func-tion for DNA–drug docking of anticancerand antiparasitic compounds based onspectral moments of 2D lattice graphsformolecular dynamics trajectories, 4461 –Prediction of telomerase inhibitory activi-ty for acridinic derivatives based on chem-ical structure, 4826 – Application ofdesirability–based multi(bi)–objectiveoptimization in the design of selectivearylpiperazine derivates for the 5–HT1Aserotonin receptor, 5045

Drug design QikProp – Mapping the ribonu-cleolytic active site of bovine seminalribonuclease. The binding of pyrimidinylphosphonucleotide inhibitors, 4496

Drug resistance – Sulphonamide–basedbombesin prodrug analogues for glutathionetransferase, useful in targeted cancerchemotherapy, 2009

Drug– and lead–like chemical space anddrug discovery – Investigation of the inci-dence of “undesirable” molecular moietiesfor high–throughput screening compoundlibraries in marketed drug compounds, 1128

Drug–like chemical space – Known drugspace as a metric in exploring the bound-aries of drug–like chemical space, 5006

Drugs – Prediction of milk/plasma concentra-tion ratios of drugs and environmental pol-lutants, 2452 – Synthesis and antimycobac-terial activity of N'–[(E)–(monosubstitut-ed–benzylidene)]–2–pyrazinecarbohy-drazide derivatives, 4954

DTZ323 – Mechanistic aspects of benzoth-iazepines: A class of antiarrhythmic drugs,1

Dual 5–HT1A/SERT activity – Novel4–aryl–pyrido[1,2–c]pyrimidines with dualSSRI and 5–HT1A activity: Part 2, 4702

dUTP nucleotidohydrolase – Design, synthe-sis and evaluation of novel uracil acetamidederivatives as potential inhibitors ofPlasmodium falciparum dUTP nucleotido-hydrolase, 678

Dynamic SIMS imaging – Unusual cellularuptake of cytotoxic4–hydroxymethyl–3–aminoacridine, 4758

EE (trans), Z (cis) isomers – Synthesis, photo-

chemical E (trans)�Z (cis) isomerizationand antimicrobial activity of2–chloro–5–methylpyridine–3–olefinderivatives, 4661

EAC – Possible anticancer agents: QSARanalogs of glutamamide: Synthesis andpharmacological activity of 1,5–N,N'–dis-ubstituted–2–(substituted benzenesulpho-nyl) glutamamides, 70

EDDA–type ligands – Palladium(II) com-plexes with R2edda–derived ligands. Part II.Synthesis, characterization and in vitro anti-tumoral studies of R2eddip esters and palla-dium(II) complexes, 3452

Efflux pump inhibitors – Quantitative struc-ture–activity relationship (QSAR) of arylalkenyl amides/imines for bacterial effluxpump inhibitors, 229 – Quantitative struc-ture activity relationship (QSAR) of piper-ine analogsfor bacterial NorA efflux pumpinhibitors, 4128

Efflux pump – Evaluation of substrate andinhibitor properties of a novel MDR modu-lator H17 towards transmembrane effluxpumps, 3060

EGF–R – Design, synthesis and characteriza-tion of N9/N7–substituted 6–aminopurinesas VEGF–R and EGF–R inhibitors, 1788

EGFR – Discovering novelquercetin–3–O–amino acid–esters as a newclass of Src tyrosine kinase inhibitors, 1982– 5–Benzylidene–hydantoins: Synthesis andantiproliferative activity on A549 lung can-cer cell line, 3471

eHiTS – CoMFA, LeapFrog and blind dock-ing studies on sulfonanilide derivatives act-ing as selective aromatase expression regu-lators, 3445

Ehrlich ascites carcinoma (EAC) – Novelmodified steroid derivatives ofandrostanolone as chemotherapeuticanti–cancer agents, 3936

Electron spray ionization mass spectrome-try – Studies on self–aggregation of anthra-cycline drugs by restrained moleculardynamics approach using nuclear magneticresonance spectroscopy supported byabsorption, fluorescence, diffusion orderedspectroscopy and mass spectrometry, 1437

Electronic structure – Computational studyof the electronic structure characterizationof a novelanti–inflammatory tripeptidederived from monocyte locomotioninhibitoryfactor (MLIF)–pentapeptide, 3114

Electrostatic attachment –Generation–dependent encapsulation/elec-trostatic attachment of phenobarbital mole-

Page 27: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5157

cules by poly(amidoamine) dendrimers:Evidence from 2D–NOESY investigations,2219

Embryonic development – Synthesis andbiological evaluation of cytotoxic propertiesof stilbene–based resveratrol analogs, 701

Enaminone esters – Synthesis, antibacterialand anticonvulsant evaluations of somecyclic enaminones, 967

Enaminonitriles – Enaminonitrile in hetero-cyclic synthesis: Synthesis and antimicro-bial evaluation of some new pyrazole, isox-azole and pyrimidine derivatives incorpo-rating a benzothiazole moiety, 4813

Enantiomeric pair – Chiral 3–(4,5–dihy-drooxazol–2–yl)phenyl alkylcarbamates asnovel FAAH inhibitors: Insight into FAAHenantioselectivity by molecular docking andinteraction fields, 4179

Enantiomers – Synthesis and adrenolyticactivity of1–(1H–indol–4–yloxy)–3–(2–(2–methoxyphenoxy)ethylamino)propan–2–ol analogsand its enantiomers. Part 2, 5103

Enantioselective synthesis – Design, synthe-sis and evaluation of tetrahydropyran basedCOX–1/–2 inhibitors, 1278

Enantioselectivity – Synthesis, characterisa-tion and in vitro cytotoxicity studies of aseries of chiral platinum(II) complexesbased on the 2–aminomethylpyrrolidine lig-and: X–ray crystal structure of[ P t C l 2 ( R – d i m e p y r r ) ](R–dimepyrr=N–dimethyl–2(R)–aminomethylpyrrolidine), 2807

Encapsulation – Generation–dependentencapsulation/electrostatic attachment ofphenobarbital molecules by poly(ami-doamine) dendrimers: Evidence from2D–NOESY investigations, 2219

Endocannabinoid – The synthesis and bio-logical evaluation of para–substituted phe-nolic N–alkyl carbamates as endocannabi-noid hydrolyzing enzyme inhibitors, 2994

Enoyl–ACP reductase – Synthesis, antituber-cular activity and docking study of novelcyclic azole substituted diphenyl etherderivatives, 492

Enoyl–acyl carrier protein reductase –Design and in silico screening of combina-torial library of antimalarial analogs of tri-closan inhibiting Plasmodium falciparumenoyl–acyl carrier protein reductase, 3009

Entamoeba histolytica – Synthesis, spectralstudies and antiamoebic activity of new1 – N – s u b s t i t u t e dthiocarbamoyl–3–phenyl–2–pyrazolines,417 – New derivatives of 3,5–substitut-ed–1,4,2–dioxazoles: Synthesis and activityagainst Entamoeba histolytica, 926 –Antiamoebic coumarins from the root barkof Adina cordifolia and their new thiosemi-carbazone derivatives, 2252 – Synthesis andin vitro trichomonicidal, giardicidal andamebicidal activity of N–acetamide(sulfon-amide)–2–methyl–4–nitro–1H–imidazoles,2975 – Computational study of the electron-ic structure characterization of anovelanti–inflammatory tripeptide derivedfrom monocyte locomotion inhibitoryfactor(MLIF)–pentapeptide, 3114 – Synthesis,

characterization, antiamoebic activity andtoxicity of novel bisdioxazole derivatives,4747

Enzymatic kinetics – Molecular modelingand inhibition of phospholipase A2 by poly-hydroxy phenolic compounds, 312

Enzyme histochemistry – Synthesis and useo f4–peptidylhydrazido–N–hexyl–1,8–naph-thalimides as fluorogenic histochemicalsubstrates for dipeptidyl peptidase IV andtripeptidyl peptidase I, 384

Enzyme inhibition – 10H–Phenothiazines: Anew class of enzyme inhibitors for inflam-matory diseases, 197 – On designingnon–saccharide, allosteric activators ofantithrombin, 2626 – Mapping the ribonu-cleolytic active site of bovine seminalribonuclease. The binding of pyrimidinylphosphonucleotide inhibitors, 4496

Enzyme – Steroidal lactones as inhibitors of17�–hydroxysteroid dehydrogenase type 5:Chemical synthesis, enzyme inhibitoryactivity, and assessment of estrogenic andandrogenic activities, 632

Enzyme–activated prodrug –Sulphonamide–based bombesin prodruganalogues for glutathione transferase, usefulin targeted cancer chemotherapy, 2009

Enzymes and enzyme reactions – Towardsan efficient prodrug of the alkylatingmetabolite monomethyltriazene: Synthesisand stability of N–acylamino acid deriva-tives of triazenes, 1049

Epidermal growth factor receptor –Synthesis and characterization of rheniumand technetium–99m tricarbonyl complexesbearing the 4–[3–bromophenyl]quinazolinemoiety as a biomarker for EGFR–TK imag-ing, 4021

Epigenetics – Reactivity of isothiazolones andisothiazolone–1–oxides in the inhibition ofthe PCAF histone acetyltransferase, 4855

Epilepsy – Synthesis and anticonvulsantactivity of some new bishydrazones derivedfrom 3,4–dipropyloxythiophene, 3672

Erythroid differentiation – Synthesis of gly-cose carbamides and evaluation of theinduction of erythroid differentiation ofhuman erythroleukemic K562 cells, 745

ES/MS – Synthesis and biochemical evalua-tion of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

Escherichia coli – Examination of growthinhibitory properties of synthetic chalconesfor which antibacterial activity was predict-ed, 2211 – A novel and efficient one stepsynthesis of 2–amino–5–cyano–6–hydroxy–4–aryl pyrimidines and theiranti–bacterial activity, 2651 – Synthesis andantibacterial activity of some new heterocy-cles incorporating phthalazine, 4448

Ester prodrugs – To determine the cytotoxic-ity of chlorambucil and one of itsnitro–derivatives, conjugated to prasteroneand pregnenolone, towards eight humancancer cell–lines, 2944

Estradiol – Synthesis, evaluation and 3DQSAR analysis of novel estradiol–RGDoctapeptide conjugates with oral anti–osteo-porosis activity, 1689

Estrogen receptor beta – Bibenzyl– and stil-bene–core compounds with non–polar link-er atom substituents as selective ligands forestrogen receptor beta, 3412 – Phenethylpyridines with non–polar internal substitu-tents as selective ligands for estrogen recep-tor beta, 3560

Estrogen receptor – Bibenzyl– andstilbene–core compounds with non–polarlinker atom substituents as selective ligandsfor estrogen receptor beta, 3412 – Phenethylpyridines with non–polar internal substitu-tents as selective ligands for estrogen recep-tor beta, 3560

Ethidium bromide – Synthesis andDNA–binding studies of two ruthenium(II)complexes of an intercalating ligand, 2044

Ethyl bromohydroxycinnamates – Newinsights into the antioxidant activity ofhydroxycinnamic acids: Synthesis andphysicochemical characterization of novelhalogenated derivatives, 2092

Ethylene glycol – Synthesis and evaluation ofin vitro anti–microbial and anti–tubercularactivity of 2–styryl benzimidazoles, 4244

Euphorbia cornigera Boiss – Bio–activecompounds from Euphorbia cornigeraBoiss, 3188

Euphorbiaceae – Bio–active compounds fromEuphorbia cornigera Boiss, 3188

EVA – A QSAR study on relationship betweenstructure of sulfonamides and their carbonicanhydrase inhibitory activity using theeigenvalue (EVA) method, 3439

Eye drops – Highly sensitive spectrofluori-metric determination of lomefloxacin inspiked human plasma, urine and pharma-ceutical preparations, 3402

FFAAH inhibitor – Chiral 3–(4,5–dihydrooxa-

zol–2–yl)phenyl alkylcarbamates as novelFAAH inhibitors: Insight into FAAH enan-tioselectivity by molecular docking andinteraction fields, 4179

FAAH – Synthesis and pharmacological eval-uation of sulfamide–based analogues ofanandamide, 4889

Factor Xa inhibitor – Design of novelaminopyrrolidine factor Xa inhibitors froma screening hit, 2787

Famotidine – PEGylated PPI dendritic archi-tectures for sustained delivery of H2 recep-tor antagonist, 1155

FA–MLR – Comparative chemometric mod-eling of cytochrome 3A4 inhibitory activityof structurally diverse compounds usingstepwise MLR, FA–MLR, PLS, GFA,G/PLS and ANN techniques, 2913

Farnesyltransferase inhibitors – 3D–QSARwith the aid of pharmacophore search anddocking–based alignments for farnesyl-transferase inhibitors, 4070

FASGAI – A set of new amino acid descrip-tors applied in prediction of MHC class Ibinding peptides, 1144

Fatty acid amide hydrolase – The synthesisand biological evaluation of para–substitut-ed phenolic N–alkyl carbamates as endo-cannabinoid hydrolyzing enzyme inhibitors,

Page 28: Chal Micro

5158 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

2994 – Chiral 3–(4,5–dihydrooxazol–2–yl)phenyl alkylcarbamates as novel FAAHinhibitors: Insight into FAAH enantioselec-tivity by molecular docking and interactionfields, 4179

FeCl3 – Design and one–pot synthesis of�–aminophosphonates andbis(�–aminophosphonates) by iron(III)chloride and cytotoxic activity, 4266

Fenbufen – Fenbufen based 3–[5–(substitutedaryl)–1,3,4–oxadiazol–2–yl]–1–(biphenyl–4–yl)propan–1–ones as safer antiinflamma-tory and analgesic agents, 3798

Fibrates – Design, synthesis and hypolipi-demic activity of novel 2–(m–tolyloxy)isobutyric acid derivatives, 2679

Fibrillogenesis – Synthesis and activity of fib-rillogenesis peptide inhibitors related to the17–21 �–amyloid sequence, 179

Fibrin – Computational modeling and surfaceplasmon resonance analyses in the assess-ment of peptide ligands interacting with fib-rin �(312–324) epitope, 2128

Fibrosis – Synthesis and biological evaluationof benzenesulfonamide–substituted4–(6–alkylpyridin–2–yl)–5–(quinox-alin–6–yl)imidazoles as transforminggrowth factor–� type 1 receptor kinaseinhibitors, 568

First principle – First–principle,structure–based prediction of hepatic meta-bolic clearance values in human, 1600

Flavone – Synthesis of 6–aminomethyl deriv-atives of benzopyran–4–one with dual bio-logical properties: Anti–inflammatory–anal-gesic and antimicrobial, 4896

Flavonoid – Stimulatory effect of api-genin–6–C–�–l–fucopyranoside on insulinsecretion and glycogen synthesis, 4668

Flavonoids – Synthesis and antitumor activityof novel dithiocarbamate substitutedchromones, 3687

Flexible docking – Natural polyprenylatedbenzophenones inhibiting cysteine and ser-ine proteases, 1230

Flourescence – Synthesis and characterizationof dinuclear macrocyclic cobalt(II), cop-per(II) and zinc(II) complexes derived from2,2,2',2'–S,S[bis(bis–N,N–2–thiobenzimida-zolyloxalato–1,2–ethane)]: DNA bindingand cleavage studies, 834

Flow cytometry – Dideoxy fluoro–ketopyra-nosyl nucleosides as potent antiviral agents:Synthesis and biological evaluation of 2,3–and 3,4–dideoxy–3–fluoro–4– and–2–keto–�–d–glucopyranosyl derivativesof N4–benzoyl cytosine, 2696

Fluconazole – Design, synthesis and biologi-cal evaluation of novel nitrogen and sulfurcontaining hetero–1,4–naphthoquinones aspotent antifungal and antibacterial agents,3130

Fluorescence assay – Synthesis and activityof fibrillogenesis peptide inhibitors relatedto the 17–21 �–amyloid sequence, 179

Fluorescence property – Synthesis, crystalstructure, antioxidant activities andDNA–binding studies of the Ln(III) com-plexes with 7–methoxychromone–3–car-baldehyde–(4'–hydroxy) benzoyl hydra-zone, 2425

Fluorescence quantum yield – An in vitrocharacterization study of new near infrareddyes for molecular imaging, 3496

Fluorescence resonance energy transfer –Fluorescence spectroscopic investigation ofthe interaction between chloramphenicoland lysozyme, 4083

Fluorescence spectroscopy – Studies on theinteraction of caffeine with bovine hemo-globin, 2100 – Fluorescence spectroscopicinvestigation of the interaction betweenchloramphenicol and lysozyme, 4083

Fluorimetry – Highly sensitive spectrofluori-metric determination of lomefloxacin inspiked human plasma, urine and pharma-ceutical preparations, 3402

Fluorinated docetaxel analogues – Design,synthesis and biological evaluation of novelfluorinated docetaxel analogues, 482

Fluorinated surfactants – Enhanced activityof fluorinated quaternary ammonium sur-factants against Pseudomonas aeruginosa,1615

Fluorinated ureas – Synthesis and anticanceractivity ofN–bis(trifluoromethyl)alkyl–N'–thiazolyland N–bis(trifluoromethyl)alkyl–N'–ben-zothiazolyl ureas, 4944

Fluorogenic substrates – Synthesis and useo f4–peptidylhydrazido–N–hexyl–1,8–naph-thalimides as fluorogenic histochemicalsubstrates for dipeptidyl peptidase IV andtripeptidyl peptidase I, 384

Fluoroquinolone – Synthesis and in vitroantibacterial activity of 7–(4–alkoxyimi-no–3–amino–3–methylpiperidin–1–yl)fluo-roquinolone derivatives, 4063 – Synthesisand antitubercular activity of palladium andplatinum complexes with fluoroquinolones,4107

Fmoc–based dipeptides – Design and synthe-sis of new N–(fluorenyl–9–methoxycar-bonyl) (Fmoc)–dipeptides as anti–inflam-matory agents, 1933

Folate derivatives – Novel8–deaza–5,6,7,8–tetrahydroaminopterinderivatives as dihydrofolate inhibitor:Design, synthesis and antifolate activity,764

Fragrant compounds – Microwave assistedsynthesis of unsaturated jasmone hetero-cyclic analogues as new fragrant sub-stances, 3032

Free radical – Captopril and 6–mercaptop-urine: Whose SH possesses higher antioxi-dant ability?, 4841

Free radical–scavenging effects – Synthesisof novel trans–stilbene derivatives andevaluation of their potent antioxidant andneuroprotective effects, 3166

Free radicals – Anti–trypanosomatid benzo-furoxans and deoxygenated analogues:Synthesis using polymer–supported triph-enylphosphine, biological evaluation andmechanism of action studies, 5055

FT–Raman – Synthesis, Raman, FT–IR,NMR spectroscopic characterization,antimicrobial activity, cytotoxicity andDNA binding of new mixed aza–oxo–thiamacrocyclic compounds, 4681

Fujita–Ban analysis – Synthesis and sero-tonin receptor activity of the arylpiperazinealkyl/propoxy derivatives of new azatricy-cloundecanes, 152

Fulleropyrrolidine – Fullerene derivatizeds–triazine analogues as antimicrobialagents, 2178

Furanone – Synthesis and pharmacologicalevaluation of 2(3H)–furanones and2(3H)–pyrrolones, combining analgesic andanti–inflammatory properties with reducedgastrointestinal toxicity and lipid peroxida-tion, 2636

Furin – Modeling the activity of furininhibitors using artificial neural network,1664

Furocoumarins – Synthesis and anti–inflam-matory evaluation of novel angularly or lin-early fused coumarins, 5012

Furopyrrolopyrazinone – Synthesis of newdipyrrolo– and furopyrrolopyrazinonesrelated to tripentones and their biologicalevaluation as potential kinases (CDKs1–5,GSK–3) inhibitors, 708

Furoquinoline – Condensed 1,4–dihydropy-ridines with various esters and their calciumchannel antagonist activities, 2052

Fused–ring systems – Synthesis and antitu-moral activity of novel thiazolobenzotria-zole, thiazoloindolo[3,2–c]quinoline andquinolinoquinoline derivatives, 3858

GG/PLS – Exploring QSAR and QAAR for

inhibitors of cytochrome P450 2A6 and2A5 enzymes using GFA and G/PLS tech-niques, 1941

G0–G1 arrest – Synthesis and antiprolifera-tive activity of3–amino–N–phenyl–1H–indazole–1–car-boxamides, 165

G2/M arrest – Novel naphthalimide deriva-tives as potential apoptosis–inducingagents: Design, synthesis and biologicalevaluation, 4674

Galanthamine derivative – Design, synthesisand evaluation of galanthamine derivativesas acetylcholinesterase inhibitors, 772

Gallium complexes – Gallium(III) complexesof 2–pyridineformamide thiosemicar-bazones: Cytotoxic activity against malig-nant glioblastoma, 1870

Gambogic acid derivatives – Studies onchemical structure modification and biologyof a natural product, Gambogic acid (I):Synthesis and biological evaluation of oxi-dized analogues of gambogic acid, 2611

Gametocytes – Primaquine revisited sixdecades after its discovery, 937

Gametocytocidal activity – Primaquinedipeptide derivatives bearing an imidazo-lidin–4–one moiety at the N–terminus aspotential antimalarial prodrugs, 2506

GA–PLS – A set of new amino acid descrip-tors applied in prediction of MHC class Ibinding peptides, 1144

Gastric toxicity – Synthesis and investigationof anti–inflammatory activity and gastriculcerogenicity of novel nitric oxide–donat-ing pyrazoline derivatives, 3068

Page 29: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5159

Gatifloxacin – Synthesis and antibacterialactivity of nitroaryl thiadiazole–gatifloxacinhybrids, 1205

GBSA – Computational modeling and surfaceplasmon resonance analyses in the assess-ment of peptide ligands interacting with fib-rin �(312–324) epitope, 2128

Gem–diol – Dideoxy fluoro–ketopyranosylnucleosides as potent antiviral agents:Synthesis and biological evaluation of 2,3–and 3,4–dideoxy–3–fluoro–4– and–2–keto–�–d–glucopyranosyl derivativesof N4–benzoyl cytosine, 2696

Gene expression – Histone deacetylaseinhibitor prodrugs in nanoparticle vectorenhanced gene expression in human cancercells, 4603

Gene expression programming – Predictingthe activity of drugs for a group of imida-zopyridine anticoccidial compounds, 4044

Genetic algorithms – Application of geneticalgorithm–support vector machine(GA–SVM) for prediction of BK–channelsactivity, 5023

Genetic function algorithm – Quantitativestructure–activity relationship (QSAR) ofaryl alkenyl amides/imines for bacterialefflux pump inhibitors, 229

Genetic function approximation (GFA) –Quantitative structure–activity relationshipanalysis of aryl alkanol piperazine deriva-tives with antidepressant activities, 4367

Genetic partial least squares (G/PLS) –Quantitative structure–activity relationshipanalysis of aryl alkanol piperazine deriva-tives with antidepressant activities, 4367

Genotoxicity – Cytotoxic and genotoxiceffects of [Ru(phi)3]2� evaluated byAmes/Salmonella and MTT methods, 2601

GFA – Exploring QSAR and QAAR forinhibitors of cytochrome P450 2A6 and2A5 enzymes using GFA and G/PLS tech-niques, 1941 – Comparative chemometricmodeling of cytochrome 3A4 inhibitoryactivity of structurally diverse compoundsusing stepwise MLR, FA–MLR, PLS, GFA,G/PLS and ANN techniques, 2913

GI50 values – Synthesis and antitumor activi-ty studies of some new fused 1,2,4–triazolederivatives carrying 2,4–dichloro–5–fluo-rophenyl moiety, 5066

GIAO calculations – The structure ofRimonabant in the solid state and in solu-tion: An experimental and theoretical study,1864

Giardia intestinalis – Synthesis and in vitrotrichomonicidal, giardicidal and amebicidalactivity ofN–acetamide(sulfonamide)–2–methyl–4–nitro–1H–imidazoles, 2975

Gliclazide – The metabolism of CYP2C9 andCYP2C19 for gliclazide by homology mod-eling and docking study, 854

Glide – Knowledge based identification ofMAO–B selective inhibitors using pharma-cophore and structure based virtual screen-ing models, 3584

Glioblastoma – Gallium(III) complexes of2–pyridineformamide thiosemicarbazones:Cytotoxic activity against malignantglioblastoma, 1870

Glutamamide – Possible anticancer agents:QSAR analogs of glutamamide: Synthesisand pharmacological activity of1,5–N,N'–disubstituted–2–(substituted ben-zenesulphonyl) glutamamides, 70

Glutathione transferase –Sulphonamide–based bombesin prodruganalogues for glutathione transferase, usefulin targeted cancer chemotherapy, 2009

GlycineB–iGluR–NMDA – Molecular orbitaldifferentiation of agonist and antagonistactivity in the GlycineB–iGluR–NMDAreceptor, 2960

Glycogen Synthase Kinase 3�� – Fragmentand knowledge–based design of selectiveGSK–3�� inhibitors using virtual screeningmodels, 2361

Glycogen synthesis – Stimulatory effect ofapigenin–6–C–�–l–fucopyranoside oninsulin secretion and glycogen synthesis,4668

Glycolamide – Synthesis and evaluation of invitro anti–tuberculosis activity of N–substi-tuted glycolamides, 289

Glycolipid – Total synthesis and anticanceractivity of highly potent novel glycolipidderivatives, 3120

Glycosidopyrimido[4,5–b]–quinolines –New acyclic nucleosides analogues aspotential analgesic, anti–inflammatory,anti–oxidant and anti–microbial derivedfrom pyrimido[4,5–b]quinolines, 1427

Glycosyl amino ester – Synthesis and antitu-bercular screening of imidazole derivatives,3350

Glycosylation – Total synthesis and anti-cancer activity of highly potent novel gly-colipid derivatives, 3120

G–quadruplex ligand – Synthesis and bio-logical evaluation of novel 4,5–bis(dialky-laminoalkyl)–substituted acridines as potenttelomeric G–quadruplex ligands, 3880

G–quartet – Prediction of telomeraseinhibitory activity for acridinic derivativesbased on chemical structure, 4826

Gold – Contact–active microbicidal gold sur-faces using immobilization of quaternaryammonium thiol derivatives, 4227

GOLD – Receptor–based 3D–QSAR studiesof checkpoint Wee1 kinase inhibitors, 1383

Gossypol aza–derivatives – Synthesis, crys-tal structures and antibacterial activity stud-ies of aza–derivatives of phytoalexin fromcotton plant – gossypol, 4393

gp120 inhibitors – Docking and 3D–QSARstudies of BMS–806 analogs as HIV–1gp120 entry inhibitors, 3524

GPCR – Homology modeling of MCH1receptor and validation by docking/scoringand protein–aligned CoMFA, 2583

Graebe–Ullmann – Synthesis and antitu-moral activity of novel thiazolobenzotria-zole, thiazoloindolo[3,2–c]quinoline andquinolinoquinoline derivatives, 3858

Granulation – Evaluation of in vivowound–healing potential of2–[4–(2,4–dimethoxy–benzoyl)–phe-noxy]–1–[4–(3–piperidin–4–yl–propyl)–piperidin–1–yl]–ethanone derivatives, 3158

Graph theory – Scoring function forDNA–drug docking of anticancer and

antiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Green chemistry – Improved synthesis ofseven aromatic Baylis–Hillman adducts(BHA): Evaluation against Artemia salinaLeach. and Leishmania chagasi, 1726

GRIND – 2D– and 3D–QSAR of Tocainideand Mexiletine analogues acting as Nav1.4channel blockers, 1477 – GRIND–based3D–QSAR and CoMFA to investigate top-ics dominated by hydrophobic interactions:The case of hERG K� channel blockers,1926

Growth inhibitory – Synthesis of new chiral2,5–disubstituted 1,3,4–thiadiazoles pos-sessing �–butenolide moiety and prelimi-nary evaluation of in vitro anticancer activ-ity, 3340

GSH – Hydroxychalcones induce apoptosis inB16–F10 melanoma cells via GSH and ATPdepletion, 1630 – Synthesis and biochemicalevaluation of a cyclic RGD oxorhenium com-plex as new ligand of �V�3 integrin, 3394

GSK–3 – Synthesis of new dipyrrolo– andfuropyrrolopyrazinones related to tripen-tones and their biological evaluation aspotential kinases (CDKs1–5, GSK–3)inhibitors, 708

Guttiferone A – Natural polyprenylated ben-zophenones inhibiting cysteine and serineproteases, 1230

HH. polyri urease – Amines and oximes derived

from deoxybenzoins as Helicobacter pyloriurease inhibitors, 2246

H3 receptor antagonist – Heterocyclicreplacement of the central phenyl core ofdiamine–basedhistamine H3 receptor antag-onists, 4413

H3–Antagonists – Non–imidazole histamineH3 ligands, Part IV: SAR of 1–[2–thia-zol–5–yl–(2–aminoethyl)]–4–n–propy-lpiperazine derivatives, 1674

HaCaT – Structure–activity relationship ofseco–tanapartholides isolated from Achilleafalcata for inhibition of HaCaT cell growth,3794

Haemolysis – Cationic surfactants fromlysine: Synthesis, micellization and biologi-cal evaluation, 1884

Haemolytic activity – Dialkylamino andnitrogen heterocyclic analogues of hexade-cylphosphocholine and cetyltrimetylammo-nium bromide: Effect of phosphate groupand environment of the ammonium cationon their biological activity, 4970

Halogen atoms and drug development/dis-covery – Known drug space as a metric inexploring the boundaries of drug–likechemical space, 5006

Halogen–metal exchange – Synthesis of �receptor ligands with unsymmetrical spiroconnection of the piperidine moiety, 4306

Hartree Fock – Mechanistic aspects of ben-zothiazepines: A class of antiarrhythmicdrugs, 1

HATU – Synthesis and biochemical evalua-tion of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

Page 30: Chal Micro

5160 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

HDAC inhibitor – Novel amide derivativesas inhibitors of histone deacetylase: Design,synthesis and SAR, 1067

HDAC – Histone deacetylase inhibitor pro-drugs in nanoparticle vector enhanced geneexpression in human cancer cells, 4603

HeLa and HCT–15 cell lines – Synthesis ofbenzamide derivatives of anacardic acid andtheir cytotoxic activity, 2711

Hela cells – Synthesis of new chiral 2,5–dis-ubstituted 1,3,4–thiadiazoles possessing�–butenolide moiety and preliminary evalu-ation of in vitro anticancer activity, 3340 –Synthesis and evaluation of anti–tumoractivities of N4 fatty acyl amino acid deriv-atives of 1–�–arabinofuranosylcytosine,3596

Hemoglobin – Synthesis and antimalarialactivity of pyrazolo and pyrimido benzoth-iazine dioxide derivatives, 1303

Heparin – On designing non–saccharide,allosteric activators of antithrombin, 2626

Hepatic metabolic clearance – First–princi-ple, structure–based prediction of hepaticmetabolic clearance values in human, 1600

Hepatitis C – Cyclic phosphoramidates asprodrugs of 2'–C–methylcytidine, 3765

Hepatocarcinogenic – Development ofQSAR models for predicting hepatocarcino-genic toxicity of chemicals, 3658

Hepatoma (HepG2) – Novel modified steroidderivatives of androstanolone as chemother-apeutic anti–cancer agents, 3936

Hepatoma – The preparation and in vitroantiproliferative activity of phthalimidebased ketones on MDAMB–231 andSKHep–1 human carcinoma cell lines, 2736

Hepatotoxicity – Synthesis and pharmacolog-ical evaluation of N–phenyl–acetamide sul-fonamides designed as novel non–hepato-toxic analgesic candidates, 3612

HEPES – Synthesis and biochemical evalua-tion of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

hERG – GRIND–based 3D–QSAR andCoMFA to investigate topics dominated byhydrophobic interactions: The case ofhERG K� channel blockers, 1926

Herpes Simplex – Structure–activity relation-ships for dipeptide prodrugs of acyclovir:Implications for prodrug design, 2339

Hesperetin hydrazone – Synthesis, character-ization, DNA binding properties and antiox-idant activity of Ln(III) complexes withhesperetin–4–one–(benzoyl) hydrazone,4585

Heteroarylacetic acids – Design, synthesisand molecular modeling study of acylated1,2,4–triazole–3–acetates with potentialanti–inflammatory activity, 117

Heterocycle – Novel 4H–1,3,4–oxadi-azin–5(6H)–ones with hydrophobic andlong alkyl chains: Design, synthesis, andbioactive diversity on inhibition ofmonoamine oxidase, chitin biosynthesis andtumor cell, 2113 – Synthesis and anti–HIVactivity evaluation of 2–(4–(naph-thalen–2–yl)–1,2,3–thiadiazol–5–ylthio)–N–acetamides as novel non–nucleosideHIV–1 reverse transcriptase inhibitors,4648

Heterocycles – Novel modified steroid deriv-atives of androstanolone as chemotherapeu-tic anti–cancer agents, 3936

Heterocyclic analogues – Microwave assistedsynthesis of unsaturated jasmone hetero-cyclic analogues as new fragrant sub-stances, 3032

Heterocyclic compounds – Synthesis andcharacterization of new Pt(II) and Pd(II)complexes with 2–quinolinecarboxaldehydeselenosemicarbazone: Cytotoxic activityevaluation of Cd(II), Zn(II), Ni(II), Pt(II)and Pd(II) complexes with heteroaromaticselenosemicarbazones, 1623

Heterocyclic derivatives – Synthesis andevaluation of a novel series of heterocyclicoleanolic acid derivatives with anti–osteo-clast formation activity, 2796

Heterocyclic replacement – Heterocyclicreplacement of the central phenyl core ofdiamine–basedhistamine H3 receptor antag-onists, 4413

Hexahydroquinoline – Condensed 1,4–dihy-dropyridines with various esters and theircalcium channel antagonist activities, 2052

Hexestrol – Bibenzyl– and stilbene–core com-pounds with non–polar linker atom sub-stituents as selective ligands for estrogenreceptor beta, 3412 – Phenethyl pyridineswith non–polar internal substitutents as selec-tive ligands for estrogen receptor beta, 3560

High–throughput screening – A new type offive–membered heterocyclic inhibitors ofbasic metallocarboxypeptidases, 3266

HipHop – Important pharmacophoric featuresof pan PPAR agonists: Common chemicalfeature analysis and virtual screening, 3488

Histamine H3–receptor – Non–imidazolehistamine H3 ligands, Part IV: SAR of1–[2–thiazol–5–yl–(2–aminoethyl)]–4–n–propylpiperazine derivatives, 1674

Histamine – Heterocyclic replacement of thecentral phenyl core of diamine–basedhista-mine H3 receptor antagonists, 4413

Histone acetyltransferase – Reactivity ofisothiazolones and isothiazolone–1–oxidesin the inhibition of the PCAF histone acetyl-transferase, 4855

Histone deacetylase inhibitor – Histonedeacetylase inhibitor prodrugs in nanoparti-cle vector enhanced gene expression inhuman cancer cells, 4603

Histone deacetylase inhibitors – Design,synthesis and preliminary biological evalu-ation of N–hydroxy–4–(3–phenyl-propanamido)benzamide (HPPB) deriva-tives as novel histone deacetylase inhibitors,4470

Histone deacetylase – Design, synthesis, andevaluation of biphenyl–4–yl–acrylohydrox-amic acid derivatives as histone deacetylase(HDAC) inhibitors, 1900

Histone deacetylases enzyme – 3D–QSARstudies of HDACs inhibitors using pharma-cophore–based alignment, 2868

HIV – Activity and molecular modeling of anew small molecule active againstNNRTI–resistant HIV–1 mutants, 5117

HIV–1 integrase inhibitors – Synthesis andanti–HIV–1 integrase activities of3–aroyl–2,3–dihydro–1,1–dioxo–1,4,2–ben

zodithiazines, 190 – Synthesis andanti–HIV–1 integrase activity of modifieddinucleotides, 5029

HIV–1 integrase – Multivariate QSAR studyof 4,5–dihydroxypyrimidine carboxamidesas HIV–1 integrase inhibitors, 3577 –Docking–based 3D–QSAR study of HIV–1integrase inhibitors, 4276

HIV–1 – Synthesis and in vitro anti–HIV eval-uation of a new series of 6–arylmethyl–sub-stituted S–DABOs as potential non–nucleo-side HIV–1 reverse transcriptase inhibitors,1016 – Novel modifications in the series ofO–(2–phthalimidoethyl)–N–substitutedthiocarbamates and their ring–opened con-geners as non–nucleoside HIV–1 reversetranscriptase inhibitors, 1650 –Thiocarbamates as non–nucleoside HIV–1reverse transcriptase inhibitors:Docking–based CoMFA and CoMSIAanalyses, 2059 – Parallel synthesis, molecu-lar modelling and further structure–activityrelationship studies of new acylthiocarba-mates as potent non–nucleoside HIV–1reverse transcriptase inhibitors, 2190 –Synthesis and anti–HIV activity evaluationof 2–(4–(naphthalen–2–yl)–1,2,3–thiadia-zol–5–ylthio)–N–acetamides as novelnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 4648

HIV–1 non–nucleoside reverse transcrip-tase inhibitors – QSAR models for2–amino–6–arylsulfonylbenzonitriles andcongeners HIV–1 reverse transcriptaseinhibitors based on linear and nonlinearregression methods, 2158

HIV–1 protease inhibitor HOE/BAY–793 –3D–QSAR CoMFA/CoMSIA models basedon theoretical active conformersofHOE/BAY–793 analogs derived fromHIV–1 protease inhibitor complexes, 4344

HIV–1 protease – Synthesis and evaluation ofA–seco type triterpenoids foranti–HIV–1protease activity, 4112

HIV–1 RT – QSAR studies for diarylpyrim-idines against HIV–1 reverse transcriptasewild–type and mutant strains, 625

HIV–1wt RT assay – Activity and molecularmodeling of a new small molecule activeagainst NNRTI–resistant HIV–1 mutants,5117

HIV–2 – Synthesis and in vitro anti–HIV eval-uation of a new series of 6–arylmethyl–sub-stituted S–DABOs as potential non–nucleo-side HIV–1 reverse transcriptase inhibitors,1016

HIV–RT – Synthesis, HIV–RT inhibitoryactivity and SAR of 1–benzyl–1H–1,2,3–tri-azole derivatives of carbohydrates, 373

HLA–A*0201 – A set of new amino aciddescriptors applied in prediction of MHCclass I binding peptides, 1144

HL–60 cells – Copper(II) and uranyl(II) com-plexes with acylthiosemicarbazide:Synthesis, characterization, antibacterialactivity and effects on the growth ofpromyelocytic leukemia cells HL–60, 3323– Synthesis and evaluation of anti–tumoractivities of N4 fatty acyl amino acid deriv-atives of 1–�–arabinofuranosylcytosine,3596

Page 31: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5161

HM – Prediction of CCR5 receptor bindingaffinity of substituted 1–(3,3–diphenyl-propyl)–piperidinyl amides and ureas basedon the heuristic method, support vectormachine and projection pursuit regression,25

HOMO – Molecular orbital differentiation ofagonist and antagonist activity in theGlycineB–iGluR–NMDA receptor, 2960

Homology model – Identification of putativesteroid–binding sites in human ABCB1 andABCG2, 3601

Homology modeling – Homology modelingof MCH1 receptor and validation by dock-ing/scoring and protein–aligned CoMFA,2583

Homophenylalanine – Synthesis andimmunosuppressive activity ofcyclolinopeptide A analogues containinghomophenylalanine, 3731

Homopiperazines – 1,4–Diazepanes derivedfrom (S)–serine – Homopiperazines withimproved �1 (sigma) receptor affinity andselectivity, 519

Hot plate – Synthesis and antinociceptiveactivities of some pyrazoline derivatives,2606

Houttuynin – Synthesis and antibacterialevaluation of novel 4–alkyl substitutedphenyl �–aldehyde ketone derivatives,1737

HPLC – Spectrophotometric and HPLC deter-minations of anti–diabetic drugs, rosiglita-zone maleate and metformin hydrochloride,in pure form and in pharmaceutical prepara-tions, 4998

HPPB – Design, synthesis and preliminarybiological evaluation ofN–hydroxy–4–(3–phenylpropanamido)ben-zamide (HPPB) derivatives as novel histonedeacetylase inhibitors, 4470

HQSAR – 2D– and 3D–QSAR studies on 54anti–tumor Rubiaceae–type cyclopeptides,3425

Human carboxypeptidase B – A new type offive–membered heterocyclic inhibitors ofbasic metallocarboxypeptidases, 3266

Human colon carcinoma – New antimalarialand cytotoxic 4–nerolidylcatechol deriva-tives, 2731

Human leukemia –(±)–3,4–Dihydroxy–8,9–methylene-dioxypterocarpan and derivatives:Cytotoxic effect on human leukemia celllines, 920

Human myeloblastic leukemia – New anti-malarial and cytotoxic 4–nerolidylcatecholderivatives, 2731

Human nervous system cancer – New anti-malarial and cytotoxic 4–nerolidylcatecholderivatives, 2731

Human neutrophils – Oligomeric formylpep-tide activity on human neutrophils, 4926

Human tumor cell lines – Novel derivativesof 6–mercaptopurine: Synthesis, characteri-zation and antiproliferative activities ofS–allylthio–mercaptopurines, 541

Hybrid benzofuroxans – Anti–trypanoso-matid benzofuroxans and deoxygenatedanalogues: Synthesis using polymer–sup-ported triphenylphosphine, biological eval-

uation and mechanism of action studies,5055

Hybrid molecules – Hybrid moleculesbetween benzenesulfonamides and activeantimicrobial benzo[d]isothiazol–3–ones,2741

Hydantoin – 5–Benzylidene–hydantoins:Synthesis and antiproliferative activity onA549 lung cancer cell line, 3471

Hydrazine derivatives – Synthesis andvasodilatory activity of some amide deriva-tives of 6–(4–carboxymethy-loxyphenyl)–4,5–dihydro–3(2H)–pyridazi-none, 4441

Hydrazine hydrate – Synthesis of somenovel bioactive 4–oxy/thiosubstituted–1H–pyrazol–5(4H)–ones viaefficient cross–Claisen condensation, 3852

Hydrazone – Synthesis, spectral characteriza-tion, in–vitro microbiological evaluationand cytotoxic activities of novel macro-cyclic bis hydrazone, 3552

Hydrazones – Synthesis of some new4–styryltetrazolo[1,5–a]quinoxaline and1–substituted–4–styryl[1,2,4]triazolo[4,3–a]quinoxaline derivatives as potent anticon-vulsants, 1135 – Novel pyridazine deriva-tives: Synthesis and antimicrobial activityevaluation, 1989 – Synthesis of newacridines and hydrazones derived fromcyclic �–diketone for cytotoxic and antivi-ral evaluation, 3680

Hydrogen bonding – Prediction of convul-sant activity of gases and vapors, 885

Hydrolytic cleavage – Hydrolytic cleavage ofDNA by urea–bridged macrocyclicpolyamines, 5090

Hydrophobicity index – QSAR studies fordiarylpyrimidines against HIV–1 reversetranscriptase wild–type and mutant strains,625

Hydrophobicity – Larvicidal activities ofsome organotin compounds on mosquitolarvae: A QSAR study, 260 – A QSAR studyfor the cytotoxic activities of taxoids againstmacrophage (M)–like cells, 274

Hydroxamic acid – Novel amide derivativesas inhibitors of histone deacetylase: Design,synthesis and SAR, 1067

Hydroxycarbamidoylmethyl – Synthesis,analgesic and anti–inflammatory activitiesof novel 3–(4–acetamido–benzyl)–5–substi-tuted–1,2,4–oxadiazoles, 794

Hydroxychalcones – Hydroxychalconesinduce apoptosis in B16–F10 melanomacells via GSH and ATP depletion, 1630

Hydroxyethylamine – Synthesis, antimalarialevaluation and molecular modeling studiesof hydroxyethylpiperazines, potentialaspartyl protease inhibitors, Part 2, 3816

Hydroxyethylpiperazine – Synthesis andantimalarial activity of hydroxyethylpiper-azine derivatives, 1363

Hydroxysteroid dehydrogenase – Steroidallactones as inhibitors of 17�–hydroxys-teroid dehydrogenase type 5: Chemical syn-thesis, enzyme inhibitory activity, andassessment of estrogenic and androgenicactivities, 632

Hypertension – Synthesis and vasodilatoryactivity of some amide derivatives of

6–(4–carboxymethyloxyphenyl)–4,5–dihy-dro–3(2H)–pyridazinone, 4441

Hypervalent iodine – Synthesis and antibac-terial activity of some new2,3–dimethoxy–3–hydroxy–2–(1–phenyl–3–aryl–4–pyrazolyl)chromanones, 1763

Hypochlorous – Investigation of the antioxi-dant properties of some new 4–hydroxy-coumarin derivatives, 3077

HypoGen model – Discovery of potentialZAP–70 kinase inhibitors: Pharmacophoredesign, database screening and dockingstudies, 4793

HypoGen – Fragment and knowledge–baseddesign of selective GSK–3� inhibitorsusing virtual screening models, 2361

Hypolipidemic – Design, synthesis andhypolipidemic activity of novel 2–(m–toly-loxy) isobutyric acid derivatives, 2679 –Design, synthesis and hypolipidemic activi-ty of novel 2–(naphthalen–2–yloxy)propi-onic acid derivatives as desmethyl fibrateanalogs, 3973

Hypotensive activity – Design, synthesis andpharmacological evaluation of new1–[3–(4–arylpiperazin–1–yl)–2–hydroxy–propyl]–3,3–diphenylpyrrolidin–2–onederivatives with antiarrhythmic, antihyper-tensive, and �–adrenolytic activity, 3994

IIbuprofen – Regioselective reaction:

Synthesis and pharmacological study ofMannich bases containing ibuprofen moi-ety, 3697

IBX – Natural tanshinone–likeheterocyclic–fused ortho–quinones fromregioselective Diels–Alder reaction:Synthesis and cytotoxicity evaluation, 3915

IL–2 – Rare dipeptide and urea derivativesfrom roots of Moringa oleifera as potentialanti–inflammatory and antinociceptiveagents, 432

IL–6 – Rare dipeptide and urea derivativesfrom roots of Moringa oleifera as potentialanti–inflammatory and antinociceptiveagents, 432

Imaging – Simple synthesis of carbon–11labeled styryl dyes as new potential PETRNA–specific, living cell imaging probes,2300

Imidazo fused – Design, synthesis, struc-ture–activity relationship and antibacterialactivity series of novel imidazo fusedquinolone carboxamides, 1570

Imidazo[1,2–a]pyridine – Physicochemicalproperties and membrane interactions ofanti–apoptotic derivatives 2–(4–fluo-rophenyl)–3–(pyridin–4–yl)imidazo[1,2–a]pyridine depending on the hydroxyalky-lamino side chain length and conformation:An NMR and ESR study, 3509

Imidazo[1,2–c]pyrimidine – Design, synthe-sis and antimycobacterial activity of somenovel imidazo[1,2–c]pyrimidines, 3837

Imidazo[2,1–b][1,3,4]thiadiazoles –Synthesis and antimicrobial studies of novelmethylene bridged benzisoxazolyl imida-zo[2,1–b][1,3,4]thiadiazole derivatives,2828

Page 32: Chal Micro

5162 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Imidazo[2,1–f]theophyllines – Synthesis andpreliminary pharmacological evaluation ofimidazo[2,1–f]purine–2,4–dione deriva-tives, 4288

Imidazole – Anti–oxidant, anti–fungal andanti–leishmanial activities ofn o v e l 3 – [ 4 – ( 1 H – i m i d a z o l – 1 – y l )phenyl]prop–2–en–1–ones, 4654

Imidazoles – Convenient one–pot synthesis ofnovel 2–substituted benzimidazoles,tetrahydrobenzimidazoles and imidazolesand evaluation of their in vitro antibacterialand antifungal activities, 1751 – Synthesisand antitubercular screening of imidazolederivatives, 3350

Imidazolidin derivatives – Synthesis andevaluation of structurally constrained imi-dazolidin derivatives as potent dipeptidylpeptidase IV inhibitors, 3318

Imidazolidineiminodithiones – Synthesis,characterization and derivatization of somenovel types of mono– and bis–imidazo-lidineiminothiones and imidazolidineimin-odithiones with antitumor, antiviral, anti-bacterial and antifungal activities – part I,4315

Imidazolidineiminothiones – Synthesis,characterization and derivatization of somenovel types of mono– and bis–imidazo-lidineiminothiones and imidazolidineimin-odithiones with antitumor, antiviral, anti-bacterial and antifungal activities – part I,4315

Imidazolidin–4–ones – Primaquine dipeptidederivatives bearing an imidazolidin–4–onemoiety at the N–terminus as potential anti-malarial prodrugs, 2506

Imidazoquinazoline derivatives –2,3–Disubstituted 8–arylamino–3H–imida-zo[4,5–g]quinazolines: A novel class ofantitumor agents, 448

Imidazoquinoxalines – Newimidazo[1,2–a]quinoxaline derivatives:Synthesis and in vitro activity againsthuman melanoma, 3406

Imiquimod – New imidazo[1,2–a]quinoxa-line derivatives: Synthesis and in vitroactivity against human melanoma, 3406

Immobilized artificial membrane chro-matography – Prediction of volume of dis-tribution values in human using immobi-lized artificial membrane partitioning coef-ficients, the fraction of compound ionizedand plasma protein binding data, 4455

Immune suppression – Synthesis andimmunosuppressive activity ofcyclolinopeptide A analogues containinghomophenylalanine, 3731

Immunosuppression –4–Phenoxybutoxy–substituted heterocycles– A structure–activity relationship study ofblockers of the lymphocyte potassium chan-nel Kv1.3, 1838

IMR–32 – Possible anticancer agents: QSARanalogs of glutamamide: Synthesis andpharmacological activity of 1,5–N,N'–dis-ubstituted–2–(substituted benzenesulpho-nyl) glutamamides, 70

In silico docking – Application of 3D QSARCoMFA/CoMSIA and in silico dockingstudies on novel renin inhibitors against car-

diovascular diseases, 3703In silico prediction – First–principle, struc-

ture–based prediction of hepatic metabolicclearance values in human, 1600

In silico screening – Design and in silicoscreening of combinatorial library of anti-malarial analogs of triclosan inhibitingPlasmodium falciparum enoyl–acyl carrierprotein reductase, 3009

In vitro activity – Newimidazo[1,2–a]quinoxaline derivatives:Synthesis and in vitro activity againsthuman melanoma, 3406

In vitro and in vivo antitumor activity – Invitro and in vivo antitumor activity of plat-inum(II) complexes with thiosemicar-bazones derived from 2–formyl and2–acetyl pyridine and containing ring incor-porated at N(4)–position: Synthesis, spec-troscopic study and crystal structure of plat-inum(II) complexes with thiosemicar-bazones, potential anticancer agents, 1296

In vitro antioxidant activity – Synthesis ofnovel benzo[h]quinolines: Wound healing,antibacterial, DNA binding and in vitroantioxidant activity, 981

In vitro assay – Antiplasmodial and antitry-panosomal activities of aminobicy-clo[2.2.2]octyl �–aminoalkanoates, 736

In vitro interaction – Antimalarial pharmaco-dynamics of chalcone derivatives in combi-nation with artemisinin against Plasmodiumfalciparum in vitro, 3388

In vitro – Evaluation of the local anaestheticactivity of 3–aminobenzo[d]isothiazolederivatives using the rat sciatic nervemodel, 473 – Search for new pharma-cophores for antimalarial activity. Part III:Synthesis and bioevaluation of new6–thioureido–4–anilinoquinazolines, 4404

In vitro – Synthesis and in vitro anti–HIVevaluation of a new series of 6–aryl-methyl–substituted S–DABOs as potentialnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 1016

In vitro/in vivo correlations (IVIVC) –Didanosine ester prodrugs: Synthesis, albu-min binding properties and pharmacokinet-ic studies in rats, 3874

In vivo fluorescence imaging – An in vitrocharacterization study of new near infrareddyes for molecular imaging, 3496

In vivo – Search for new pharmacophores forantimalarial activity. Part III: Synthesis andbioevaluation of new 6–thioureido–4–anili-noquinazolines, 4404

In vivo studies – Synthesis, characterizationand antidiabetic properties of N1–2,4–dihy-droxybenzylidene–N4–2–hydroxybenzyli-dene–S–methyl–thiosemicarbazidato–oxo-vanadium(IV), 818

Indane dimers – A series of 1, 2–coupledindane dimers with mast cell stabilisationand smooth muscle relaxation properties,5018

Indan–1–one derivatives – Synthesis andbioactivity of substituted indan–1–ylide-neaminoguanidine derivatives, 3771

Indanone – Design, synthesis and AChEinhibitory activity of indanone and auronederivatives, 7

Indigoids – Synthesis, kinase inhibitorypotencies and in vitro antiproliferativeactivity of isoindigo and 7'–azaisoindigoderivatives substituted by Sonogashiracross–coupling, 2705

Indole analogues – Synthesis and preliminaryscreening of novel indole–3–methanaminesas 5–HT4 receptor ligands, 2952

Indole ligands – Development of CoMFA andCoMSIA models of affinity and selectivityfor indole ligands of cannabinoid CB1 andCB2 receptors, 2482

Indolocarbazoles – A three–step synthesisfrom rebeccamycin of an efficient check-point kinase 1 inhibitor, 2234

Indoloquinoline – Synthesis and antitumoralactivity of novel thiazolobenzotriazole, thi-azoloindolo[3,2–c]quinoline and quinolino-quinoline derivatives, 3858

Inducible NOS – Phenylpyrrole derivatives asneural and inducible nitric oxide synthase(nNOS and iNOS) inhibitors, 2655

Inflammatory bowel disease – Colon–specif-ic mutual amide prodrugs of 4–aminosali-cylic acid for their mitigating effect onexperimental colitis in rats, 131 – Synthesis,kinetic studies and pharmacological evalua-tion of mutual azo prodrugs of 5–aminosal-icylic acid for colon–specific drug deliveryin inflammatory bowel disease, 3922

Inflammatory diseases – A novel QSARmodel for predicting the inhibition ofCXCR3 receptor by 4–N–aryl–[1,4]diazepane ureas, 877

Infrared spectra – Synthesis and spectro-scopic studies of biologically active com-pounds derived from oxalyldihydrazide andbenzil, and their Cr(III), Fe(III) and Mn(III)complexes, 1731

Ingenol esters – Bio–active compounds fromEuphorbia cornigera Boiss, 3188

InhA – Discovery of potential new InhAdirect inhibitors based on pharmacophore-and 3D–QSAR analysis followed by in sili-co screening, 3718

Inhalation anesthesia – Prediction of convul-sant activity of gases and vapors, 885

Inhibitor – Steroidal lactones as inhibitors of17�–hydroxysteroid dehydrogenase type 5:Chemical synthesis, enzyme inhibitoryactivity, and assessment of estrogenic andandrogenic activities, 632 –Structure–based virtual screening for identi-fication of novel 11�–HSD1 inhibitors,1167 – Discovering novelquercetin–3–O–amino acid–esters as a newclass of Src tyrosine kinase inhibitors, 1982– Synthesis and evaluation of A–seco typetriterpenoids for anti–HIV–1protease activi-ty, 4112

Inhibitors – Classification models forCYP450 3A4 inhibitors and non–inhibitors,2354 – Phenylpyrrole derivatives as neuraland inducible nitric oxide synthase (nNOSand iNOS) inhibitors, 2655 – Synthesis andevaluation of pyrido[1,2–a]pyrimidines asinhibitors of nitric oxide synthases, 2877

Inhibitors of NF–��B and AP–1 mediatedtranscriptional activation – Design, synthe-sis and characterization of novel2–(2,4–disubstituted–thiazole–5–yl)–3–ar

Page 33: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5163

yl–3H–quinazoline–4–one derivatives asinhibitors of NF–��B and AP–1 mediatedtranscription activation and as potentialanti–inflammatory agents, 2184

Inhibitory activity – Synthesis and evaluationof a novel series of heterocyclic oleanolicacid derivatives with anti–osteoclast forma-tion activity, 2796

Inhibitory – Synthesis, Raman, FT–IR, NMRspectroscopic characterization, antimicro-bial activity, cytotoxicity and DNA bindingof new mixed aza–oxo–thia macrocycliccompounds, 4681

iNOS – Synthesis and biological evaluation ofcurcumin–like diarylpentanoid analoguesfor anti–inflammatory, antioxidant andanti–tyrosinase activities, 3195

Insilico analysis – Synthesis and in vitro anti-tumor activities of novel 4–anilinoquinazo-line derivatives, 3046

Insulin – Stimulatory effect ofapigenin–6–C–�–l–fucopyranoside oninsulin secretion and glycogen synthesis,4668

Integrin – Synthesis and biochemical evalua-tion of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

Interaction energy – Molecular structure andstability of perindopril erbumine andperindopril l–arginine complexes, 101

Intercalation – Novel N–(3–carboxyl–9–ben-zyl–�–carboline–1–yl)ethylamino acids:Synthesis, anti–tumor evaluation, intercalat-ing determination, 3D QSAR analysis anddocking investigation, 4153

Intercalative mode – Synthesis and charac-terization of the Zn(II) and Cu(II)piperidinyl isoeuxanthone complexes:DNA–binding and cytotoxic activity, 4509

Intercalator–dinucleotide conjugates –Synthesis and anti–HIV–1 integrase activityof modified dinucleotides, 5029

Intramolecular lactonization – Synthesis ofnovel 3–(aryl)benzothieno[2,3–c]pyran–1–ones from Sonogashira products andintramolecular cyclization: Antitumoralactivity evaluation, 1893

Inverse QSAR – Application ofdesirability–based multi(bi)–objective opti-mization in the design of selectivearylpiperazine derivates for the 5–HT1Aserotonin receptor, 5045

Invertebrates – Aziridine alkaloids as poten-tial therapeutic agents, 3373

Iodobenzene diacetate – Synthesis and anti-bacterial activity of some new2,3–dimethoxy–3–hydroxy–2–(1–phenyl–3–aryl–4–pyrazolyl)chromanones, 1763 –Organoiodine (III)–mediated synthesis of3–aryl/heteroaryl–5,7–dimethyl–1,2,4–tria-zolo[4,3–c]pyrimidines as antibacterialagents, 2260

Ion–pair extraction – Spectrophotometricand HPLC determinations of anti–diabeticdrugs, rosiglitazone maleate and metforminhydrochloride, in pure form and in pharma-ceutical preparations, 4998

Isochroman–3–(S)–carboxylic acid –Synthesis and evaluation of some novelisochroman carboxylic acid derivatives aspotential anti–diabetic agents, 3147

Isoflavone – Synthesis and anti–osteoporoticevaluation of certain 3–amino–2–hydrox-ypropoxyisoflavone derivatives, 3621

Isoform selectivity – Synthesis and evalua-tion of pyrido[1,2–a]pyrimidines asinhibitors of nitric oxide synthases, 2877

Isoindigos – Synthesis, kinase inhibitorypotencies and in vitro antiproliferativeactivity of isoindigo and 7'–azaisoindigoderivatives substituted by Sonogashiracross–coupling, 2705

Isoniazid – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Design, synthesis of 8–alkoxy–5,6–dihy-dro–[1,2,4]triazino[4,3–a]quinolin–1–oneswith anticonvulsant activity, 1265 –Preparation and antitubercular activities invitro and in vivo of novel Schiff bases ofisoniazid, 4169

Isonicotinic acid hydrazide – Synthesis ofsome new 1,2,4–triazoles, their Mannichand Schiff bases and evaluation of theirantimicrobial activities, 1057 – Synthesis ofsome new 1,2,4–triazoles starting fromisonicotinic acid hydrazide and evaluationof their antimicrobial activities, 4362

Isoprenyl – Pentacyclo–undecane derivedcyclic tetra–amines: Synthesis and evalua-tion as potent anti–tuberculosis agents, 4297

Isoquinoline – The synthesis of N–phe-noxyethyl–1–substituted–1,2,3,4–tetrahy-droisoquinolines and their �1–adrenoceptorblocking activity, 1271 – Solution–phaseparallel synthesis and evaluation of anticon-vulsant activity of N–substituted–3,4–dihy-droisoquinoline–2(1H)–carboxamides, 1349

Isothiazolone – Reactivity of isothiazolonesand isothiazolone–1–oxides in the inhibitionof the PCAF histone acetyltransferase, 4855

Isothiazolone–1–oxide – Reactivity of isoth-iazolones and isothiazolone–1–oxides in theinhibition of the PCAF histone acetyltrans-ferase, 4855

Isothiocyanates – Synthesis, characterizationand in vitro antimicrobial activity of novel2–thioxo–4–thiazolidinones and4,4'–bis(2–thioxo–4–thiazolidinone–3–yl)diphenylsulfones, 4148 – Anti–nitric oxideproduction activity of isothiocyanates corre-lates with their polar surface area rather thantheir lipophilicity, 4931

Isoxazolines – Synthesis, optimization andstructure–activity relationships of 3,5–dis-ubstituted isoxazolines as new anti–tubercu-losis agents, 460

JJasmone – Microwave assisted synthesis of

unsaturated jasmone heterocyclic analoguesas new fragrant substances, 3032

JHU75528 – Analogs of JHU75528, a PETligand for imaging of cerebral cannabinoidreceptors (CB1): Development of ligandswith optimized lipophilicity and bindingaffinity, 593

KK562 cell line – Design, synthesis and struc-

ture–activity relationships of antiprolifera-

tive 1,3–disubstituted urea derivatives,453

K562 cells – Synthesis of glycose carbamidesand evaluation of the induction of erythroiddifferentiation of human erythroleukemicK562 cells, 745

KB cell line – Design, synthesis and struc-ture–activity relationships of antiprolifera-tive 1,3–disubstituted urea derivatives, 453

KB3 cell line – Discovery of a new family ofbis–8–hydroxyquinoline substituted benzy-lamines with pro–apoptotic activity in can-cer cells: Synthesis, structure–activity rela-tionship, and action mechanism studies, 558

Ketene N,S–acetal – Synthesis and antibac-terial activity of some new heterocyclesincorporating phthalazine, 4448

Ketene S,S–diacetal – Synthesis and antibac-terial activity of some new heterocyclesincorporating phthalazine, 4448

Keto–carbazole – Regioselective synthesisand antimicrobial screening of novel keto-carbazolodispiropyrrolidine derivatives,959

Keto–enamine Schiff bases –Antidyslipidemic and antioxidative activi-ties of 8–hydroxyquinoline derived novelketo–enamine Schiffs bases, 1813

Kinase inhibitor – Pharmacophore modelingand virtual screening for the discovery ofnew transforming growth factor–� type Ireceptor (ALK5) inhibitors, 4259

Kinase inhibitors – Synthesis, kinaseinhibitory potencies and in vitro antiprolif-erative activity of isoindigo and 7'–aza-isoindigo derivatives substituted bySonogashira cross–coupling, 2705

Kinetics – Towards an efficient prodrug of thealkylating metabolite monomethyltriazene:Synthesis and stability of N–acylamino acidderivatives of triazenes, 1049

Knoevenagel reaction – Synthesis of novelthiazolone–based compounds containingpyrazoline moiety and evaluation of theiranticancer activity, 1396

Known drug space – Known drug space as ametric in exploring the boundaries ofdrug–like chemical space, 5006

Kv1.3 – 4–Phenoxybutoxy–substituted hete-rocycles – A structure–activity relationshipstudy of blockers of the lymphocyte potas-sium channel Kv1.3, 1838

LL1210 – Cytotoxic activity and chemical reac-

tivity of cis–platinum(II) and trans–palladi-um(II) complexes with diethyl (pyridinyl-methyl)phosphates, 660

Lactone – Steroidal lactones as inhibitors of17�–hydroxysteroid dehydrogenase type 5:Chemical synthesis, enzyme inhibitoryactivity, and assessment of estrogenic andandrogenic activities, 632

Lanthanide complex – Synthesis, crystal struc-ture, antioxidant activities and DNA–bindingstudies of the Ln(III) complexes with7–methoxychromone–3–carbaldehyde–(4'–hydroxy) benzoyl hydrazone, 2425

Lapachol – A macrolactone frombenzo[a]phenazine with potent activityagainst Mycobacterium tuberculosis, 2334

Page 34: Chal Micro

5164 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Larvae – Larvicidal activities of some organ-otin compounds on mosquito larvae: AQSAR study, 260

LASSBio–1300 – Synthesis and pharmaco-logical evaluation of N–phenyl–acetamidesulfonamides designed as novel non–hepa-totoxic analgesic candidates, 3612

LC–MS – Synthesis and biochemical evalua-tion of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394

Lead optimization – Synthesis, optimizationand structure–activity relationships of3,5–disubstituted isoxazolines as newanti–tuberculosis agents, 460

LeapFrog – CoMFA, LeapFrog and blinddocking studies on sulfonanilide derivativesacting as selective aromatase expressionregulators, 3445

Left–handed polyproline II conformation –Circular dichroism studies of type III colla-gen mimetic peptides with anti– orpro–aggregant activities on human platelets,2643

Leishmania chagasi – Improved synthesis ofseven aromatic Baylis–Hillman adducts(BHA): Evaluation against Artemia salinaLeach. and Leishmania chagasi, 1726

Leishmania donovani – Phase transfer cat-alyzed synthesis of bis–quinolines:Antileishmanial activity in experimentalvisceral leishmaniasis and in vitro antibac-terial evaluation, 845 – A new series ofamodiaquine analogues modified in thebasic side chain with in vitro antileishma-nial and antiplasmodial activity, 5071

Leishmania major –Nitroimidazolyl–1,3,4–thiadiazole–basedanti–leishmanial agents: Synthesis and invitro biological evaluation, 1758

Leishmania – Scoring function for DNA–drugdocking of anticancer and antiparasiticcompounds based on spectral moments of2D lattice graphsfor molecular dynamicstrajectories, 4461

Leishmania spp – Anti–trypanosomatid ben-zofuroxans and deoxygenated analogues:Synthesis using polymer–supported triph-enylphosphine, biological evaluation andmechanism of action studies, 5055

Leishmaniasis – Synthesis, biological evalua-tion and SAR of sulfonamide 4–methoxy-chalcone derivatives with potentialantileishmanial activity, 755 – In vitro andin vivo antitrypanosomatid activity of5–nitroindazoles, 1034 – Synthesis andantileishmanial activity of novel2,4,6–trisubstituted pyrimidines and1,3,5–triazines, 2473 – Second generationof 2H–benzimidazole 1,3–dioxide deriva-tives as anti–trypanosomatid agents:Synthesis, biological evaluation, and modeof action studies, 4426

Leukemia – Synthesis, NMR characterizationand in vitro antitumor evaluation of newaminophosphonic acid diesters, 3363 –Synthesis and evaluation of anti–tumoractivities of N4 fatty acyl amino acid deriv-atives of 1–�–arabinofuranosylcytosine,3596

LFER – Prediction of CCR5 receptor bindingaffinity of substituted 1–(3,3–diphenyl-

propyl)–piperidinyl amides and ureas basedon the heuristic method, support vectormachine and projection pursuit regression,25

LIF – Synthesis, cytotoxicity and effects ofsome 1,2,4–triazole and 1,3,4–thiadiazolederivatives on immunocompetent cells, 63 –Cytotoxicity and effects of 1,10–phenan-throline and 5–amino–1,10–phenanthrolinederivatives on some immunocompetentcells, 5099

LiHMDS – Synthesis of some novel bioactive4–oxy/thio substituted–1H–pyrazol–5(4H)–ones via efficient cross–Claisen con-densation, 3852

Linear discriminant analysis – Multi–targetspectral moment: QSAR for antifungaldrugs vs. different fungi species, 4051

Linear free energy relationship – Predictionof convulsant activity of gases and vapors,885 – Prediction of milk/plasma concentra-tion ratios of drugs and environmental pol-lutants, 2452

Linezolid – Synthesis and antibacterial activi-ty of novel 5–(4–methyl–1H–1,2,3–tria-zole) methyl oxazolidinones, 3217

Lipid and triglyceride lowering activity –Novel 2–aryl–naphtho[1,2–d]oxazole deriv-atives as potential PTP–1B inhibitors show-ing antihyperglycemic activities, 109

Lipid chitosan derivatives – Mucoadjuvantproperties of lipo– and glycoconjugatedderivatives of oligochitosans, 2030

Lipid lowering activity – Antidyslipidemicand antioxidative activities of 8–hydrox-yquinoline derived novel keto–enamineSchiffs bases, 1813

Lipid peroxidation – Synthesis and pharma-cological evaluation of 2(3H)–furanonesand 2(3H)–pyrrolones, combining analgesicand anti–inflammatory properties withreduced gastrointestinal toxicity and lipidperoxidation, 2636 – Fenbufen based3–[5–(substituted aryl)–1,3,4–oxadia-zol–2–yl]–1–(biphenyl–4–yl)propan–1–ones as safer antiinflammatory and analgesicagents, 3798 – Synthesis of 6–aminomethylderivatives of benzopyran–4–one with dualbiological properties:Anti–inflammatory–analgesic and antimi-crobial, 4896

Lipid rafts – Molecular properties of psy-chopharmacological drugs determiningnon–competitive inhibition of 5–HT3Areceptors, 2667

Lipoic acid – Synthesis and evaluation of theantioxidant and anti–inflammatory activityof novel coumarin–3–aminoamides andtheir alpha–lipoic acid adducts, 3020

Lipophilicity – Antileukotrienic phenethylami-do derivatives of arylalkanoic acids in thetreatment of ulcerative colitis, 332 –Synthesis of (±)Abyssinone I and relatedcompounds: Their anti–oxidant and cytotoxicactivities, 2239 – Synthesis, physicochemicalproperties and antimicrobial activity of somenew benzimidazole derivatives, 4028

Live cell – Simple synthesis of carbon–11labeled styryl dyes as new potential PETRNA–specific, living cell imaging probes,2300

Ln(III) complexes – Synthesis, characteriza-tion, DNA binding properties and antioxi-dant activity of Ln(III) complexes with hes-peretin–4–one–(benzoyl) hydrazone, 4585

l–Proline – l–Proline–catalysed facile greenprotocol for the synthesis and antimycobac-terial evaluation of [1,4]–thiazines, 4978

l–Tryptophan – Colon–specific mutual amideprodrugs of 4–aminosalicylic acid for theirmitigating effect on experimental colitis inrats, 131

Lomefloxacin – Highly sensitive spectrofluo-rimetric determination of lomefloxacin inspiked human plasma, urine and pharma-ceutical preparations, 3402

Long–chain arylpiperazines – The influenceof an ethylene spacer on the 5–HT1A and5–HT2A receptor affinity of arylpiperazinederivatives of amides with N–acylatedamino acids and 3–differently substitutedpyrrolidine–2,5–diones, 800

Low–molecular weight chitosan –Mucoadjuvant properties of lipo– and gly-coconjugated derivatives of oligochitosans,2030

LOX – Adamantane derivatives ofthiazolyl–N–substituted amide, as possiblenon–steroidal anti–inflammatory agents,1198

LPS–induced NO generation – Synthesis ofnovel trans–stilbene derivatives and evalua-tion of their potent antioxidant and neuro-protective effects, 3166

LUMO – Molecular orbital differentiation ofagonist and antagonist activity in theGlycineB–iGluR–NMDA receptor, 2960

Luteolin derivatives – Synthesis and biologi-cal evaluation of novel luteolin derivativesas antibacterial agents, 908

Lysine – Cationic surfactants from lysine:Synthesis, micellization and biologicalevaluation, 1884

Lysosomes – Unusual cellular uptake of cyto-toxic 4–hydroxymethyl–3–aminoacridine,4758

Lysozyme – Fluorescence spectroscopicinvestigation of the interaction betweenchloramphenicol and lysozyme, 4083

Lysozyme release – Oligomeric formylpep-tide activity on human neutrophils, 4926

MM1 receptor binding – Synthesis and phar-

macological evaluation of novelN–alkyl/aryl substituted thiazolidinonearecoline analogues as muscarinic receptor1 agonist in Alzheimer’s dementia models,4848

Macrocyclic complexes – Synthesis and spec-troscopic studies of biologically active com-pounds derived from oxalyldihydrazide andbenzil, and their Cr(III), Fe(III) and Mn(III)complexes, 1731 – Antimicrobial activemacrocyclic complexes of Cr(III), Mn(III)and Fe(III) with their spectroscopicapproach, 3299

Macrocyclic compounds – Physicochemicaland biological characterization of novelmacrocycles derived from o–phthalalde-hyde, 2621

Page 35: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5165

Macrocyclic – Synthesis, Raman, FT–IR,NMR spectroscopic characterization,antimicrobial activity, cytotoxicity andDNA binding of new mixed aza–oxo–thiamacrocyclic compounds, 4681

Macrolactones – A macrolactone frombenzo[a]phenazine with potent activityagainst Mycobacterium tuberculosis, 2334

Macrolide – Synthesis and antibacterial activ-ity of novel 15–membered macrolide deriv-atives: 4"–Carbamate, 11,12–cyclic carbon-ate–4"–carbamate and 11,4"–di–O–arylcar-bamoyl analogs of azithromycin, 4010

Macrophage (M)–like cells – A QSARstudy for the cytotoxic activities of taxoidsagainst macrophage (M–like cells, 274

Magnesium oxide – A facile one–pot greensynthesis and antibacterial activity of2–amino–4H–pyrans and2–amino–5–oxo–5,6,7,8–tetrahydro–4H–chromenes, 3805

Malaria – Primaquine revisited six decadesafter its discovery, 937 – Synthesis and anti-malarial activity of hydroxyethylpiperazinederivatives, 1363 – Substituted quinolinylchalcones and quinolinyl pyrimidines as anew class of anti–infective agents, 2081 –Primaquine dipeptide derivatives bearing animidazolidin–4–one moiety at the N–termi-nus as potential antimalarial prodrugs, 2506– Design and in silico screening of combi-natorial library of antimalarial analogs oftriclosan inhibiting Plasmodium falciparumenoyl–acyl carrier protein reductase, 3009 –Recent developments in the design and syn-thesis of hybrid molecules basedon amino-quinoline ring and their antiplasmodialevaluation, 3091 – Synthesis, antimalarialevaluation and molecular modeling studiesof hydroxyethylpiperazines, potentialaspartyl protease inhibitors, Part 2, 3816

Maleimide – Synthesis and antimicrobialactivity of some new N–acyl substitutedphenothiazines, 5094

Malononitrile – Synthesis, antimicrobial andantioxidant activities of substituted pyra-zoles, isoxazoles, pyrimidine and thioxopy-rimidine derivatives, 4557

Mammalian – Evaluation of the local anaes-thetic activity of 3–aminobenzo[d]isothia-zole derivatives using the rat sciatic nervemodel, 473

Mannich base – Synthesis, pharmacologicalscreening, quantum chemical and in vitropermeability studies of N–Mannich bases ofbenzimidazoles through bovine cornea,2307 – Synthesis of some new 1,3,4–thiadi-azol–2–ylmethyl–1,2,4–triazole derivativesand investigation of their antimicrobialactivities, 2896 – Regioselective reaction:Synthesis and pharmacological study ofMannich bases containing ibuprofen moi-ety, 3697

Mannich bases – Synthesis, spectral studiesand antiamoebic activity of new 1–N–sub-stituted thiocarbamoyl–3–phenyl–2–pyra-zolines, 417 – Synthesis, characterizationand antibacterial activity of some triazoleMannich bases carrying diphenylsulfonemoieties, 3083 – Regioselective reaction:Synthesis, characterization and pharmaco-

logical studies of some new Mannich basesderived from 1,2,4–triazoles, 3784

Mannich ketone – Antifungal unsaturatedcyclic Mannich ketones and amino alco-hols: Study of mechanism of action, 1823

MAO–B – Knowledge based identification ofMAO–B selective inhibitors using pharma-cophore and structure based virtual screen-ing models, 3584

Marketed drug compounds – Known drugspace as a metric in exploring the bound-aries of drug–like chemical space, 5006

Markov model – Multi–target spectralmoment: QSAR for antifungal drugs vs. dif-ferent fungi species, 4051 – Multi–targetspectral moments for QSAR and ComplexNetworks study of antibacterial drugs, 4516

Markov models – Scoring function forDNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Mast cell stabilising activity – A series of 1,2–coupled indane dimers with mast cell sta-bilisation and smooth muscle relaxationproperties, 5018

Maximal electroshock (MES) – Synthesisand anticonvulsant activity ofN–(2–hydroxyethyl) cinnamamide deriva-tives, 3654

Maximal electroshock – Design and synthe-sis of 5–alkoxy–[1,2,4]triazolo[4,3–a]quinoline derivatives with anticonvulsantactivity, 954

Maximal electroshock seizure test –Synthesis and potential anticonvulsantactivity of new N–3–substituted 5,5–cyclo-propanespirohydantoins, 296

Maximal electroshock–induced seizures –Synthesis and anticonvulsant activity ofsome substituted 1,2,4–thiadiazoles, 1100

MCF–7 cell line – Synthesis of(±)Abyssinone I and related compounds:Their anti–oxidant and cytotoxic activities,2239

MCF–7 cells – Novel Biginelli dihydropyrim-idines with potential anticancer activity: Aparallel synthesis and CoMSIA study, 4192

MCF–7 – Synthesis and antitumor activity ofoptically active thiourea and their2–aminobenzothiazole derivatives: A novelclass of anticancer agents, 2923

MCH1R inhibitors – Homology modeling ofMCH1 receptor and validation bydocking/scoring and protein–alignedCoMFA, 2583

MDR modulator – Evaluation of substrateand inhibitor properties of a novel MDRmodulator H17 towards transmembraneefflux pumps, 3060

MDR phenotype –(±)–3,4–Dihydroxy–8,9–methylene-dioxypterocarpan and derivatives:Cytotoxic effect on human leukemia celllines, 920

MED–3DMC – MED–3DMC: A new tool togenerate 3D conformation ensembles ofsmall molecules with a Monte Carlo sam-pling of the conformational space, 1405

Melanoma – Hydroxychalcones induce apop-tosis in B16–F10 melanoma cells via GSH

and ATP depletion, 1630 – New antimalari-al and cytotoxic 4–nerolidylcatechol deriva-tives, 2731 – Dopamine– andtyramine–based derivatives of triazenes:Activation by tyrosinase and implicationsfor prodrug design, 3228 – New imida-zo[1,2–a]quinoxaline derivatives: Synthesisand in vitro activity against humanmelanoma, 3406

Melatonin – Melatonin: Quantum–chemicaland biochemical investigation of antioxi-dant activity, 2834

MES – Design, synthesis of8–alkoxy–5,6–dihydro–[1,2,4]triazino[4,3–a]quinolin–1–ones with anticonvulsantactivity, 1265 – Synthesis, anticonvulsantand CNS depressant activity of some newbioactive 1–(4–substituted–phenyl)–3–(4–oxo–2–phenyl/ethyl–4H–quina-zolin–3–yl)–urea, 4335

Metallocarboxypeptidase – A new type offive–membered heterocyclic inhibitors ofbasic metallocarboxypeptidases, 3266

Metallodrugs – Metals in anticancer therapy:Copper(II) complexes as inhibitors of the20S proteasome, 4353

Metformin – Spectrophotometric and HPLCdeterminations of anti–diabetic drugs,rosiglitazone maleate and metforminhydrochloride, in pure form and in pharma-ceutical preparations, 4998

Methicillin–resistant Staphylococcus aureus– Synthesis and in vitro antimicrobial activ-ity of some novel substituted benzimidazolederivatives having potent activity againstMRSA, 1024

Methionyl–tRNA synthetase inhibitors –2–[2–Substituted–3–(3,4–dichlorobenzy-lamino)propylamino]–1H–quinolin–4–onesas Staphylococcus aureus methionyl–tRNAsynthetase inhibitors, 239

Methylthiobenzyl moiety – Synthesis andantimicrobial activities of some new tria-zolothiadiazoles bearing 4–methylthioben-zyl moiety, 551

Mexiletine – 2D– and 3D–QSAR of Tocainideand Mexiletine analogues acting as Nav1.4channel blockers, 1477

Michael addition – Synthesis, characteriza-tion and antimicrobial activity of water sol-uble dendritic macromolecules, 1093 –Synthesis, antimicrobial and antioxidantactivities of substituted pyrazoles, isoxa-zoles, pyrimidine and thioxopyrimidinederivatives, 4557

Microbial – Synthesis, characterization, DNAcleavage and in vitro antimicrobial studies ofLa(III), Th(IV) and VO(IV) complexes withSchiff bases of coumarin derivatives, 2904

Micro–organisms – Aziridine alkaloids aspotential therapeutic agents, 3373

Micronucleus assay – Photo–inducible cyto-toxic and clastogenic activities of3,6–di–substituted acridines obtained byacylation of proflavine, 2459

Microwave assisted synthesis – Microwaveassisted synthesis of unsaturated jasmoneheterocyclic analogues as new fragrant sub-stances, 3032

Microwave irradiation – Synthesis of ami-dine and amide derivatives and their evalu-

Page 36: Chal Micro

5166 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

ation for anti–inflammatory and analgesicactivities, 1010

Microwave – New acyclic nucleosides ana-logues as potential analgesic, anti–inflam-matory, anti–oxidant and anti–microbialderived from pyrimido[4,5–b]quinolines,1427 – Diazinium salts with dihydroxyace-tophenone skeleton: Syntheses and antimi-crobial activity, 2275

Microwaves – Microwave–induced synthesisand anti–microbial activities of7,10,11,12–tetrahydrobenzo[c]acridin–8(9H)–one derivatives, 976 – Synthesis andantitumoral activity of novel thiazolobenzo-triazole, thiazoloindolo[3,2–c]quinoline andquinolinoquinoline derivatives, 3858

Milk – Prediction of milk/plasma concentra-tion ratios of drugs and environmental pol-lutants, 2452

Milk/plasma ratios – Prediction of milk/plas-ma concentration ratios of drugs and envi-ronmental pollutants, 2452

Minimal inhibitory concentration –Preparation and antimicrobial behaviour ofquaternary ammonium thiol derivatives ableto be grafted on metal surfaces, 717 –Enhanced activity of fluorinated quaternaryammonium surfactants againstPseudomonas aeruginosa, 1615

Minimal lethal concentration – Preparationand antimicrobial behaviour of quaternaryammonium thiol derivatives able to begrafted on metal surfaces, 717

Minimum inhibitory concentration –Synthesis and spectroscopic studies of bio-logically active compounds derived fromoxalyldihydrazide and benzil, and theirCr(III), Fe(III) and Mn(III) complexes,1731 – Synthesis, characterization and anti-bacterial activity of2–[1–(5–chloro–2–methoxy–phenyl)–5–methyl–1H–pyrazol–4–yl]–5–(substituted–phenyl)–[1,3,4]oxadiazoles, 4522

Minor groove binder – Design, synthesis,and anti–tumor evaluation of novel sym-metrical bis–benzimidazoles, 1808

Mitochondria – The cytotoxic properties andpreferential toxicity to tumour cells dis-played by some 2,4–bis(benzylidene)– 8 – m e t h y l – 8 – a z a b i c y c l o [ 3 . 2 . 1 ]octan–3–ones and 3,5–bis(benzylidene)–1–methyl–4–piperidones, 54

Mitochondrial dehydrogenases – Secondgeneration of 2H–benzimidazole 1,3–diox-ide derivatives as anti–trypanosomatidagents: Synthesis, biological evaluation,and mode of action studies, 4426 –Anti–trypanosomatid benzofuroxans anddeoxygenated analogues: Synthesis usingpolymer–supported triphenylphosphine,biological evaluation and mechanism ofaction studies, 5055

Mitochondrial NOS – Phenylpyrrole deriva-tives as neural and inducible nitric oxidesynthase (nNOS and iNOS) inhibitors,2655

Mixed–ligand ternary complexes –Antimicrobial and SOD activities of noveltransition metal ternary complexes of imin-odiacetic acid containing �–diimine as aux-iliary ligand, 2517

MLR–FA – QSAR modelling of pancreatic�–cell KATP channel openers R/S–3,4–dihy-dro–2,2–dimethyl–6–halo–4–(substitutedphenylaminocarbonylamino)–2H–1–ben-zopyrans using MLR–FA techniques, 359

Mode of action – Study of 5–nitroindazoles’anti–Trypanosoma cruzi mode of action:Electrochemical behaviour and ESR spec-troscopic studies, 1545

MODEL (MOlecular DEscriptor Lab)descriptors – Juglone derivatives as antitu-bercular agents: A rationale for the activityprofile, 2847

Modification – A class of novelN–(3S–1,2,3,4–tetrahydroisoquinoline–3–carbonyl)–l–amino acid derivatives: theirsynthesis, anti–thrombotic activity evalua-tion, and 3D QSAR analysis, 4904

Modified ant colony – Quantitative struc-ture–activity relationship study of serotonin(5–HT7) receptor inhibitors using modifiedant colony algorithm and adaptiveneuro–fuzzy interference system (ANFIS),1463

Modified dinucleotides – Synthesis andanti–HIV–1 integrase activity of modifieddinucleotides, 5029

Molar refractivity – Synthesis and QSARmodeling of 2–acetyl–2–ethoxycar-bonyl–1–[4(4'–arylazo)–phenyl]–N,N–dimethylaminophenyl aziridines as potentialantibacterial agents, 251 – Larvicidal activ-ities of some organotin compounds on mos-quito larvae: A QSAR study, 260 – A QSARstudy for the cytotoxic activities of taxoidsagainst macrophage (M)–like cells, 274

Molecular descriptor – Multi–target spectralmoments for QSAR and Complex Networksstudy of antibacterial drugs, 4516

Molecular descriptors – QSAR analysis ofsalicylamide isosteres with the use of quan-tum chemical molecular descriptors, 869

Molecular docking – The metabolism ofCYP2C9 and CYP2C19 for gliclazide byhomology modeling and docking study, 854– Virtual screening for Raf–1 kinaseinhibitors based on pharmacophore modelof substituted ureas, 1240 – Receptor–based3D–QSAR studies of checkpoint Wee1kinase inhibitors, 1383 – Novel modifica-tions in the series of O–(2–phthalimi-doethyl)–N–substituted thiocarbamates andtheir ring–opened congeners as non–nucleo-side HIV–1 reverse transcriptase inhibitors,1650 – Design, synthesis, and biologicalevaluation of novel triazole derivatives asinhibitors of cytochrome P45014�–demethylase, 1913 – Synthesis, phar-macological evaluation and docking studiesof new sulindac analogues, 1959 – A newtype of five–membered heterocyclicinhibitors of basic metallocarboxypeptidas-es, 3266 – New azoles with potent antifun-gal activity: Design, synthesis and molecu-lar docking, 4218

Molecular dynamics – Penetratin and deriva-tives acting as antifungal agents, 212 –Potential of mean force for Syrian hamsterprion epitope protein – Monoclonal fab 3f4antibody interaction studies, 3504 – Scoringfunction for DNA–drug docking of anti-

cancer and antiparasitic compounds basedon spectral moments of 2D lattice graphsformolecular dynamics trajectories, 4461

Molecular field analysis (MFA) –Quantitative structure–activity relationshipanalysis of aryl alkanol piperazine deriva-tives with antidepressant activities, 4367

Molecular modeling – The cytotoxic proper-ties and preferential toxicity to tumour cellsdisplayed by some 2,4–bis(benzyli-dene)–8–methyl–8–azabicyclo[3.2.1]octan–3–ones and 3,5–bis(benzyli-dene)–1–methyl–4–piperidones, 54 –Molecular modeling and inhibition of phos-pholipase A2 by polyhydroxy phenolic com-pounds, 312 – Synthesis and biologicalevaluation of a new family of anti–benzy-lanilinosulfonamides as CA IX inhibitors,511 – Analogs of JHU75528, a PET ligandfor imaging of cerebral cannabinoid recep-tors (CB1): Development of ligands withoptimized lipophilicity and binding affinity,593 – Novel 8–deaza–5,6,7,8–tetrahy-droaminopterin derivatives as dihydrofolateinhibitor: Design, synthesis and antifolateactivity, 764 – A novel QSAR model forpredicting the inhibition of CXCR3 receptorby 4–N–aryl–[1,4] diazepane ureas, 877 –Design, synthesis, and anti–tumor evalua-tion of novel symmetrical bis–benzimida-zoles, 1808 – Substituted quinazolines, part3. Synthesis, in vitro antitumor activity andmolecular modeling study of certain2–thieno–4(3H)–quinazolinone analogs,2379 – Design, synthesis and antimycobac-terial activity of some novelimidazo[1,2–c]pyrimidines, 3837 –3D–QSAR CoMFA/CoMSIA models basedon theoretical active conformersofHOE/BAY–793 analogs derived fromHIV–1 protease inhibitor complexes, 4344– Activity and molecular modeling of a newsmall molecule active againstNNRTI–resistant HIV–1 mutants, 5117

Molecular modelling – Synthesis and in vitrocysticidal activity of new benzimidazolederivatives, 1794 – GRIND–based3D–QSAR and CoMFA to investigate top-ics dominated by hydrophobic interactions:The case of hERG K� channel blockers,1926

Molecular structure – Antiviral evaluation ofN–amino–1,2,3–triazoles against Cantagalovirus replication in cell culture, 3777

Molluscicidal activity – Synthesis and mol-luscicidal activity of some new thiophene,thiadiazole and pyrazole derivatives, 1250 –Bio–active compounds from Euphorbiacornigera Boiss, 3188

Mono, bis–6–arylbenzimidazo[1,2–c]quina-zolines – Mono and bis–6–arylbenzimida-zo[1,2–c]quinazolines: A new class ofantimicrobial agents, 3330

Monoamine oxidase – Synthesis and antibac-terial activity of novel5–(4–methyl–1H–1,2,3–triazole) methyloxazolidinones, 3217

Monoglyceride lipase – The synthesis and bio-logical evaluation of para–substituted phe-nolic N–alkyl carbamates as endocannabi-noid hydrolyzing enzyme inhibitors, 2994

Page 37: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5167

Monomers – Synthesis and antimicrobialproperties of polymerizable quaternaryammoniums, 3201

Monophosphate prodrug – Cyclic phospho-ramidates as prodrugs of 2'–C–methylcyti-dine, 3765

Monosaccharides – Synthesis of glycose car-bamides and evaluation of the induction oferythroid differentiation of human ery-throleukemic K562 cells, 745

Monte Carlo method – Scoring function forDNA–drug docking of anticancer andantiparasitic compounds based on spectralmoments of 2D lattice graphsfor moleculardynamics trajectories, 4461

Morpholine – Novel4–(morpholin–4–yl)–N'–(arylidene)benzo-hydrazides: Synthesis, antimycobacterialactivity and QSAR investigations, 3954

Morpholine ring – Design, synthesis andstructure–activity relationships of antipro-liferative 1,3–disubstituted urea derivatives,453

Mosquito – Larvicidal activities of someorganotin compounds on mosquito larvae:A QSAR study, 260

MTT assay – New derivatives of 3,5–substi-tuted–1,4,2–dioxazoles: Synthesis andactivity against Entamoeba histolytica, 926– Synthesis and in vitro antiproliferativeactivity of novel 1–benzhydrylpiperazinederivatives against human cancer cell lines,1223 – Synthesis, structure and biologicalactivity of copper(II) complexes of4–(2–pyridylmethyl)–1,7–dimethyl–1,4,7–triazonane–2,6–dione and4–(2–pyridylethyl)–1,7–dimethyl–1,4,7–tri-azonane–2,6–dione, 1607 – Antiamoebiccoumarins from the root bark of Adinacordifolia and their new thiosemicarbazonederivatives, 2252 – Synthesis and biologicalactivity evaluation of 1H–benzimidazolesvia mammalian DNA topoisomerase I andcytostaticity assays, 2280 – Synthesis andantitumor activity of optically activethiourea and their 2–aminobenzothiazolederivatives: A novel class of anticanceragents, 2923 – To determine the cytotoxici-ty of chlorambucil and one of itsnitro–derivatives, conjugated to prasteroneand pregnenolone, towards eight humancancer cell–lines, 2944 – Synthesis, charac-terization, antiamoebic activity and toxicityof novel bisdioxazole derivatives, 4747

MTT–assay – Synthesis, NMR characteriza-tion and in vitro antitumor evaluation ofnew aminophosphonic acid diesters, 3363

Mucoadjuvant – Mucoadjuvant properties oflipo– and glycoconjugated derivatives ofoligochitosans, 2030

Mucosal immunization – Mucoadjuvantproperties of lipo– and glycoconjugatedderivatives of oligochitosans, 2030

Multiconformational ensemble –MED–3DMC: A new tool to generate 3Dconformation ensembles of small moleculeswith a Monte Carlo sampling of the confor-mational space, 1405

Multidrug resistance – Cytotoxicity andTOP1–targeting activity of 8– and 9–aminoderivatives of 5–butyl– and

5–(2–N,N–dimethylamino)ethyl–5H–diben-zo[c,h][1,6]naphthyridin–6–ones, 1471 –Novel topoisomerase I–targeting antitumoragents synthesized from theN,N,N–trimethylammonium derivative ofARC–111, 5H–2,3–dimethoxy–8,9–methyl-enedioxy–5–[(2–N,N,N–trimethylammoni-u m ) e t h y l ] d i b e n z o [ c , h ] [ 1 , 6 ] n a p h -thyridin–6–one iodide, 3433

Multidrug–resistant M. tuberculosis –Preparation and in vitro evaluation of ben-zylsulfanyl benzoxazole derivatives aspotential antituberculosis agents, 2286

Multilamellar vesicles – Physicochemicalproperties and membrane interactions ofanti–apoptotic derivatives 2–(4–fluo-rophenyl)–3–(pyridin–4–yl)imidazo[1,2–a]pyridine depending on the hydroxyalky-lamino side chain length and conformation:An NMR and ESR study, 3509

Multi–component reaction –Microwave–induced synthesis andanti–microbial activities of7,10,11,12–tetrahydrobenzo[c]acridin–8(9H)–one derivatives, 976 – A facile one–potgreen synthesis and antibacterial activity of2–amino–4H–pyrans and2–amino–5–oxo–5,6,7,8–tetrahydro–4H–chromenes, 3805

Multi–drug resistant tuberculosis –l–Proline–catalysed facile green protocolfor the synthesis and antimycobacterialevaluation of [1,4]–thiazines, 4978

Multi–target QSAR – Multi–target spectralmoment: QSAR for antifungal drugs vs. dif-ferent fungi species, 4051

Multiobjective optimization – Application ofdesirability–based multi(bi)–objective opti-mization in the design of selectivearylpiperazine derivates for the 5–HT1Aserotonin receptor, 5045

Mutagenicity – Lowering of 5–nitroimida-zole’s mutagenicity: Towards optimalantiparasitic pharmacophore, 653 –Cytotoxic and genotoxic effects of[Ru(phi)3]

2� evaluated by Ames/Salmonellaand MTT methods, 2601

Mutual amide prodrug – Colon–specificmutual amide prodrugs of 4–aminosalicylicacid for their mitigating effect on experi-mental colitis in rats, 131

Mutual azo prodrug – Synthesis, kineticstudies and pharmacological evaluation ofmutual azo prodrugs of 5–aminosalicylicacid for colon–specific drug delivery ininflammatory bowel disease, 3922

Mycobacterium smegmatis – l–Proline–catal-ysed facile green protocol for the synthesisand antimycobacterial evaluation of[1,4]–thiazines, 4978

Mycobacterium tuberculosis – A facile syn-thesis of�,�'–(EE)–bis(benzylidene)–cycloalka-nones and their antitubercular evaluations,1705 – Preparation and in vitro evaluationof benzylsulfanyl benzoxazole derivativesas potential antituberculosis agents, 2286 –Synthesis and antitubercular activity ofnovel 4–substitutedimidazolyl–2,6–dimethyl–N3,N5–bis-aryl–1,4–dihydropyridine–3,5–dicarboxam-

ides, 3253 – Antitumor and antimycobacte-rial activities of cyclopalladated complexes:X–ray structure of[ P d ( C 2 , N – d m b a ) ( B r ) ( t u ) ](dmba=N ,N–d ime thy lbenzy lamine ,tu=thiourea), 4611 – 1,5–Diaryl–2–ethylpyrrole derivatives as antimycobacterialagents: Design, synthesis, and microbiolog-ical evaluation, 4734 – l–Proline–catalysedfacile green protocol for the synthesis andantimycobacterial evaluation of [1,4]–thi-azines, 4978

Myocardium hypoxia – Theporphyrin–fullerene nanoparticles to pro-mote the ATP overproduction in myocardi-um: 25Mg2�–magnetic isotope effect, 1554

NN,N'–Dimethyldiiminopyrimidines –

Synthesis, antimicrobial and antioxidantactivities of substituted pyrazoles, isoxa-zoles, pyrimidine and thioxopyrimidinederivatives, 4557

N7/N9–Substituted 6–aminopurines –Design, synthesis and characterization ofN9/N7–substituted 6–aminopurines asVEGF–R and EGF–R inhibitors, 1788

Nanocapsules – An investigation into the roleof surfactants in controlling particle size ofpolymeric nanocapsules containing peni-cillin–G in double emulsion, 2392

Nano–carrier – Targeting cancer cells withbiotin–dendrimer conjugates, 862

Naphtha[1,2–d]thiazol–2–amine – Synthesisof some novel N4–(naphtha[1,2–d]thia-zol–2–yl)semicarbazides as potential anti-convulsants, 203

Naphthalene derivatives – Synthesis andantiprotozoal activities of dicationicbis(phenoxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Naphthalimide derivatives – Synthesis anduse of4–peptidylhydrazido–N–hexyl–1,8–naph-thalimides as fluorogenic histochemicalsubstrates for dipeptidyl peptidase IV andtripeptidyl peptidase I, 384

Naphthalimide – Synthesis, cytotoxicity andapoptosis of naphthalimide polyamine con-jugates as antitumor agents, 393 – Novelnaphthalimide derivatives as potential apop-tosis–inducing agents: Design, synthesisand biological evaluation, 4674

Naphthofuranoquinone – Natural tanshi-none–like heterocyclic–fusedortho–quinones from regioselectiveDiels–Alder reaction: Synthesis and cyto-toxicity evaluation, 3915

Neoglycoconjugates – Synthesis and cytotox-ic profile of glycosyl–triazole linked to1,2,4–oxadiazole moiety at C–5 through astraight–chain carbon and oxygen atoms,3571

Nerve agents – Synthesis and evaluation ofnovel bis–pyridinium oximes as reactivatorsof DFP–inhibited acetylcholinesterase,1335

Neural network – Modeling the activity offurin inhibitors using artificial neural net-work, 1664

Page 38: Chal Micro

5168 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Neural NOS – Phenylpyrrole derivatives asneural and inducible nitric oxide synthase(nNOS and iNOS) inhibitors, 2655

Neuroprotection – Synthesis of some novelN4–(naphtha[1,2–d]thiazol–2–yl)semicar-bazides as potential anticonvulsants, 203 –Synthesis of some urea and thiourea deriv-atives of 3–phenyl/ethyl–2–thioxo–2,3–dihydrothiazolo[4,5–d]pyrimidine andtheir antagonistic effects onhaloperidol–induced catalepsy and oxida-tive stress in mice, 3889

Neuroprotective activity – Synthesis of noveltrans–stilbene derivatives and evaluation oftheir potent antioxidant and neuroprotectiveeffects, 3166

Neurotoxicity – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity,954 – Synthesis and anticonvulsant activi-ty of some substituted 1,2,4–thiadiazoles,1100 – Synthesis and anticonvulsant activ-ity of N–(2–hydroxyethyl) cinnamamidederivatives, 3654 – A new class of anticon-vulsants possessing 6Hz activity:3,4–Dialkyloxy thiophene bishydrazones,4376

NF–��B – 3D–QSAR studies on theinhibitors of AP–1 and NF–��B mediatedtranscriptional activation, 2888

NHE1 inhibitors – Synthesis and bioactivityof substituted indan–1–ylideneaminoguani-dine derivatives, 3771

Nicotinic acid – Copper complexes of pyri-dine derivatives with superoxide scaveng-ing and antimicrobial activities, 3259

Nimesulide – Synthesis, antiviral and anti-cancer activity of some novel thioureasderivedfrom N–(4–nitro–2–phe-noxyphenyl)–methanesulfonamide, 3591

NIR fluorophore – An in vitro characteriza-tion study of new near infrared dyes formolecular imaging, 3496

Nitrenium ions – Known drug space as a met-ric in exploring the boundaries of drug–likechemical space, 5006

Nitric oxide – Synthesis and investigation ofanti–inflammatory activity and gastriculcerogenicity of novel nitric oxide–donat-ing pyrazoline derivatives, 3068 – Design,synthesis and pharmacological screening ofnovel nitric oxide donors containing1,5–diarylpyrazolin–3–one as nontoxicNSAIDs, 4622 – Anti–nitric oxide produc-tion activity of isothiocyanates correlateswith their polar surface area rather than theirlipophilicity, 4931

Nitric oxide synthase – Synthesis and evalu-ation of pyrido[1,2–a]pyrimidines asinhibitors of nitric oxide synthases, 2877

Nitrile oxide – A facile synthesis and antimy-cobacterial evaluation of novel spiro–pyri-do–pyrrolizines and pyrrolidines, 3821

Nitrilimines – Regioselective syntheticapproaches towards 1,2,8,9–tetraazadispiro[4.1.4.2]trideca–2,9–dien–6–ones of poten-tial antimicrobial properties, 2447

Nitro group substitution – Synthesis of someN–substituted nitroimidazole derivatives aspotential antioxidant and antifungal agents,645

Nitrobenzene – Synthesis of new 2–substitut-ed pyrido[2,3–d]pyrimidin–4(1H)–ones andtheir antibacterial activity, 1369

Nitrofuran – Synthesis and antibacterialactivity of nitroaryl thiadiazole–gatifloxacinhybrids, 1205

Nitrofurans – Synthesis, optimization andstructure–activity relationships of 3,5–dis-ubstituted isoxazolines as new anti–tubercu-losis agents, 460

Nitrogen mustards – Synthesis and in vitrocytotoxicity of 9–anilinoacridines bearingN–mustard residue on both anilino and acri-dine rings, 3056

Nitroimidazole – Synthesis of some N–substi-tuted nitroimidazole derivatives as potentialantioxidant and antifungal agents, 645 –Synthesis and antibacterial activity ofnitroaryl thiadiazole–gatifloxacin hybrids,1205 – Nitroimidazolyl–1,3,4–thiadia-zole–based anti–leishmanial agents:Synthesis and in vitro biological evaluation,1758

Nitroindazoles – In vitro and in vivo antitry-panosomatid activity of 5–nitroindazoles,1034

Nitromethane – Synthesis and antimicrobialevaluation of1–(benzofuran–2–yl)–4–nitro–3–arylbu-tan–1–ones and3–(benzofuran–2–yl)–4,5–dihydro–5–aryl–1–[4–(aryl)–1,3–thiazol–2–yl]–1H–pyra-zoles, 2632

Nitroquinolones – Synthesis and antimy-cobacterial activities of novel 6–nitro-quinolone–3–carboxylic acids, 345

Nitrothiophene – Synthesis and antibacterialactivity of nitroaryl thiadiazole–gatifloxacinhybrids, 1205

NMR – Synthesis, NMR characterization andin vitro antitumor evaluation of newaminophosphonic acid diesters, 3363 –Synthesis and biochemical evaluation of acyclic RGD oxorhenium complex as newligand of �V�3 integrin, 3394

NMR spectroscopy – Promising carbo-ranylquinazolines for boron neutron capturetherapy: Synthesis, characterization, and invitro toxicity evaluation, 409 – Synthesisand characterization of new Pt(II) andPd(II) complexes with 2–quinolinecarbox-aldehyde selenosemicarbazone: Cytotoxicactivity evaluation of Cd(II), Zn(II), Ni(II),Pt(II) and Pd(II) complexes with heteroaro-matic selenosemicarbazones, 1623

N–(3–Carboxyl–9–benzyl–��–carboline–1–yl)ethylamino acid – Novel N–(3–car-boxyl–9–benzyl–��–carboline–1–yl)ethyl-amino acids: Synthesis, anti–tumor evalua-tion, intercalating determination, 3D QSARanalysis and docking investigation, 4153

N–acyl modification – Synthesis and pharma-cokinetic evaluation of novelN–acyl–cordycepin derivatives with a nor-mal alkyl chain, 665

N–Acylhydrazone – Studies towards theidentification of putative bioactive confor-mation of potent vasodilator arylideneN–acylhydrazone derivatives, 4004

N–Acylhydrazones – Synthesis and antimy-cobacterial activity of N'–[(E)–(monosubsti-

tuted–benzylidene)]–2–pyrazinecarbohy-drazide derivatives, 4954

N–Alkylation – N1–Alkylated 3,4–dihy-dropyrimidine–2(1H)–ones: Convenientone–pot selective synthesis and evaluationof their calcium channel blocking activity,1997

N–Arachidonoylethanolamine – The synthe-sis and biological evaluation of para–sub-stituted phenolic N–alkyl carbamates asendocannabinoid hydrolyzing enzymeinhibitors, 2994

N–Arylcyanothioformanilides – Synthesis,characterization and derivatization of somenovel types of mono– and bis–imidazo-lidineiminothiones and imidazolidineimin-odithiones with antitumor, antiviral, anti-bacterial and antifungal activities – part I,4315

N–Benzyloxycarbonyl–S–phenylalanine –Synthesis, characterization and antimicro-bial activity of Co(II), Zn(II) and Cd(II)complexes withN–benzyloxycarbonyl–S–phenylalanine,1537

N–carboxymethyl imides – Synthesis andantimicrobial activity of some new N–acylsubstituted phenothiazines, 5094

N–formylmethionyl peptides – Oligomericformylpeptide activity on human neu-trophils, 4926

N–Glycolyl muramic acid – Synthesis andevaluation of in vitro anti–tuberculosisactivity of N–substituted glycolamides, 289

N–Hydroxybenzamide – Design, synthesisand preliminary biological evaluation ofN–hydroxy–4–(3–phenylpropanamido)ben-zamide (HPPB) derivatives as novel histonedeacetylase inhibitors, 4470

N–Methylpiperazine – Synthesis and spectralcharacterization of a new class ofN–(N–methylpiperazinoacetyl)–2,6–diarylpiperidin–4–ones: Antimicrobial, analgesicand antipyretic studies, 577

N–Phenethyl–2–arylacetamides –Antileukotrienic phenethylamido deriva-tives of arylalkanoic acids in the treatmentof ulcerative colitis, 332

N–Phenyl–acetamide sulfonamides –Synthesis and pharmacological evaluationof N–phenyl–acetamide sulfonamidesdesigned as novel non–hepatotoxic anal-gesic candidates, 3612

N–Phenylthioamide – Mechanism of unusualformation of 3–(5–phenyl–3H–[1,2,4]dithi-azol–3–yl)chromen–4–ones and4–oxo–4H–chromene–3–carbothioic acidN–phenylamides and their antimicrobialevaluation, 3209

N–phosphorylalkylene–3,5–bis(arylidene)piperid–4–ones – Design, cytotoxic and fluo-rescent properties of novel N–phosphory-lalkyl substituted E,E–3,5–bis(arylidene)piperid–4–ones, 2135

N–phosphorylalkylene–piperid–4–ones –Design, cytotoxic and fluorescent propertiesof novel N–phosphorylalkyl substitutedE,E–3,5–bis(arylidene)piperid–4–ones,2135

NNRTI – QSAR models for 2–amino–6–aryl-sulfonylbenzonitriles and congeners HIV–1

Page 39: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5169

reverse transcriptase inhibitors based on lin-ear and nonlinear regression methods, 2158

NNRTI resistant mutants – Activity andmolecular modeling of a new small mole-cule active against NNRTI–resistant HIV–1mutants, 5117

NNRTIs – Synthesis and anti–HIV studies of2– and 3–adamantyl–substituted thiazo-lidin–4–ones, 303 – QSAR studies fordiarylpyrimidines against HIV–1 reversetranscriptase wild–type and mutant strains,625 – Synthesis and in vitro anti–HIV eval-uation of a new series of 6–arylmethyl–sub-stituted S–DABOs as potential non–nucleo-side HIV–1 reverse transcriptase inhibitors,1016 – Synthesis and anti–HIV activityevaluation of 2–(4–(naphthalen–2–yl)–1,2,3–thiadiazol–5–ylthio)–N–acetamidesas novel non–nucleoside HIV–1 reversetranscriptase inhibitors, 4648

N–Substituted amides – Synthesis, structureelucidation and antitumour activity ofN–substituted amides of 3–(3–ethyl-thio–1,2,4–triazol–5–yl)propenoic acid,3788

NOESY – Generation–dependent encapsula-tion/electrostatic attachment of phenobarbi-tal molecules by poly(amidoamine) den-drimers: Evidence from 2D–NOESY inves-tigations, 2219

Non–invasive tail–cuff method – Synthesisand pharmacological investigation of3–(substituted 1–phenylethanone)–4–(sub-stituted phenyl)–1, 2, 3, 4–tetrahydropyrim-idine–5–carboxylates, 3645

Non–nucleoside reverse transcriptaseinhibitors (NNRTIs) – Synthesis ofalkenyldiarylmethanes (ADAMs) contain-ing benzo[d]isoxazole andoxazolidin–2–one rings, a new series ofpotent non–nucleoside HIV–1 reverse tran-scriptase inhibitors, 1210

Non–nucleoside reverse transcriptaseinhibitors – Novel modifications in theseries of O–(2–phthalimidoethyl)–N–substi-tuted thiocarbamates and their ring–openedcongeners as non–nucleoside HIV–1reverse transcriptase inhibitors, 1650 –Parallel synthesis, molecular modelling andfurther structure–activity relationship stud-ies of new acylthiocarbamates as potentnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 2190

Non–steroidal anti–inflammatory drugs(NSAIDs) – Polycyclic cage structures ascarrier molecules for neuroprotectivenon–steroidal anti–inflammatory drugs, 2577

Non–tuberculous mycobacteria –Preparation and in vitro evaluation of ben-zylsulfanyl benzoxazole derivatives aspotential antituberculosis agents, 2286

Non–ulcerogenic – Design, synthesis andpharmacological screening of novel nitricoxide donors containing 1,5–diarylpyra-zolin–3–one as nontoxic NSAIDs, 4622

Non–viral vector – Histone deacetylaseinhibitor prodrugs in nanoparticle vectorenhanced gene expression in human cancercells, 4603

Nonpungency – Synthesis and antinocicep-tive activity of capsinoid derivatives, 3345

Nonsteroidal anti–inflammatory drugs(NSAID) – The novel phosphoramidatederivatives of NSAID 3–hydroxypropy-lamides: Synthesis, cytostatic and antiviralactivity evaluations, 143

NorA – Quantitative structure activity rela-tionship (QSAR) of piperine analogsforbacterial NorA efflux pump inhibitors, 4128

Norfloxacin – Design, synthesis and in vitroantibacterial/antifungal evaluation ofnovel1–ethyl–6–fluoro–1,4–dihydro–4–oxo–7(1–piperazinyl)quinoline–3–carboxyli-cacid derivatives, 4726

Noyori catalyst – Antiproliferative activity ofarborescidine alkaloids and derivatives,3810

NPP – Identification of hydrolytically stableand selective P2Y1 receptor agonists, 1525

NSAIDs – Synthesis and pharmacologicalevaluation of a novel series of 5–(substitut-ed)aryl–3–(3–coumarinyl)–1–phenyl–2–pyrazolines as novel anti–inflammatory andanalgesic agents, 1682 – Synthesis, pharma-cological evaluation and docking studies ofnew sulindac analogues, 1959

NTPDase – Identification of hydrolyticallystable and selective P2Y1 receptor agonists,1525

Nuclear Magnetic Resonance –Physicochemical properties and membraneinteractions of anti–apoptotic derivatives2–(4–fluorophenyl)–3–(pyridin–4–yl)imi-dazo[1,2–a]pyridine depending on thehydroxyalkylamino side chain length andconformation: An NMR and ESR study,3509

Nucleoside transporter – Synthesis of aseries of N6–substituted adenosines withactivity against trypanosomatid parasites,3665

Nucleosides – Synthesis, antiviral activity,and stability of nucleoside analogs contain-ing tricyclic bases, 3845

Nucleotide–binding domain – Identificationof putative steroid–binding sites in humanABCB1 and ABCG2, 3601

Nucleotides – Identification of hydrolyticallystable and selective P2Y1 receptor agonists,1525

Nystatin – Synthesis, Raman, FT–IR, NMRspectroscopic data and antimicrobial activi-ty of mixed aza–oxo–thia macrocyclic com-pounds, 365 – Synthesis, characterizationand antimicrobial activity of water solubledendritic macromolecules, 1093

OOdor evaluation – Microwave assisted syn-

thesis of unsaturated jasmone heterocyclicanalogues as new fragrant substances, 3032

Oleanolic acid – Synthesis and evaluation ofa novel series of heterocyclic oleanolic acidderivatives with anti–osteoclast formationactivity, 2796

Oligonucleotide conjugation –Oligonucleotide–polyamine conjugates:Influence of length and position of2'–attached polyamines on duplex stabilityand antisense effect, 670

O–(2–Phthalimidoethyl)–N–arylthiocarba-mates – Novel modifications in the series of

O–(2–phthalimidoethyl)–N–substitutedthiocarbamates and their ring–opened con-geners as non–nucleoside HIV–1 reversetranscriptase inhibitors, 1650

Onion root tip assay – Anti–genotoxichydrazide from Crinum defixum, 2754

o–Phthalaldehyde – Physicochemical andbiological characterization of novel macro-cycles derived from o–phthalaldehyde,2621

OPS – Multivariate QSAR study of 4,5–dihy-droxypyrimidine carboxamides as HIV–1integrase inhibitors, 3577

Optimal descriptor – QSPR modeling bio-concentration factor (BCF) by balance ofcorrelations, 2544

Oral bioavailability – Design of novelaminopyrrolidine factor Xa inhibitors froma screening hit, 2787

Organophosphorus nerve agents – In–vitroregeneration of sarin inhibited electric eelacetylcholinesterase by bis–pyridiniumoximes bearing xylene linker, 1326

Organophosphorus pesticides – Synthesisand evaluation of novel bis–pyridiniumoximes as reactivators of DFP–inhibitedacetylcholinesterase, 1335

Organotin – Synthesis, characterization,antimicrobial and antitumor screening ofsome diorganotin(IV) complexes of2–[(9H–Purin–6–ylimino)]–phenol, 3981

Organotins – Larvicidal activities of someorganotin compounds on mosquito larvae:A QSAR study, 260

Osteoclast formation – Synthesis and evalua-tion of a novel series of heterocyclic oleano-lic acid derivatives with anti–osteoclast for-mation activity, 2796

Oxadiazole derivatives – Synthesis of novelpyrazole derivatives and evaluation of theirantidepressant and anticonvulsant activities,3480

Oxadiazoles – Synthesis and anti–inflamma-tory activity of newer quinazolin–4–onederivatives, 83

Oxaliplatin derivatives – Cytotoxic, antioxi-dant activities and structure activity rela-tionship of some newly synthesized ter-penoidal oxaliplatin analogs, 901

Oxa–Heck reaction –(±)–3,4–Dihydroxy–8,9–methylene-dioxypterocarpan and derivatives:Cytotoxic effect on human leukemia celllines, 920

Oxazole – Novel 2,4,5–trisubstituted oxazolederivatives: Synthesis and antiproliferativeactivity, 3930

Oxazolidinone – Synthesis and antibacterialactivity of novel5–(4–methyl–1H–1,2,3–triazole) methyloxazolidinones, 3217

Oxazolidinones – Synthesis, antibacterial andanticonvulsant evaluations of some cyclicenaminones, 967

Oxiconazole – Tetrahydronaphthyl azoleoxime ethers: The conformationally rigidanalogues of oxiconazole as antibacterials,437

Oxidation – Synthesis of new 2–substitutedpyrido[2,3–d]pyrimidin–4(1H)–ones andtheir antibacterial activity, 1369

Page 40: Chal Micro

5170 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Oxidative stress – Synthesis and antioxidantpotential of novel synthetic benzophenoneanalogues, 2724 – Melatonin:Quantum–chemical and biochemical inves-tigation of antioxidant activity, 2834 – BlueCrO5 assay: A novel spectrophotometricmethod for the evaluation of the antioxidantand oxidant capacity of various biologicalsubstances, 4162

Oximes – Amines and oximes derived fromdeoxybenzoins as Helicobacter pylori ure-ase inhibitors, 2246

Oxoaporphine derivatives – Synthesis, bio-logical evaluation and molecular modelingof oxoisoaporphine and oxoaporphinederivatives as new dual inhibitors of acetyl-cholinesterase/butyrylcholinesterase, 2523

Oxoisoaporphine derivatives – Synthesis,biological evaluation and molecular model-ing of oxoisoaporphine and oxoaporphinederivatives as new dual inhibitors of acetyl-cholinesterase/butyrylcholinesterase, 2523

Oxygen heterocycle –Bromoalkoxyxanthones as promising anti-tumor agents: Synthesis, crystal structureand effect on human tumor cell lines, 3830

PP. aeruginosa – Synthesis, structure and struc-

ture–activity relationship analysis of3–tert–butoxycarbonyl–2–arylthiazoli-dine–4–carboxylic acid derivatives aspotential antibacterial agents, 3903

P2Y1/2/4/6 receptor – Identification ofhydrolytically stable and selective P2Y1receptor agonists, 1525

Palladium complex – Synthesis and antitu-bercular activity of palladium and platinumcomplexes with fluoroquinolones, 4107

Palladium(II) complexes – Antitumour activ-ity of novel 1,10–phenanthroline and5–amino–1,10–phenanthroline derivatives,2720

Palladium(II) complexes – Cytotoxic activityand chemical reactivity of cis–platinum(II)and trans–palladium(II) complexes withdiethyl (pyridinylmethyl)phosphates, 660

Palladium(II) complexes – Cytotoxicity andeffects of 1,10–phenanthroline and5–amino–1,10–phenanthroline derivativeson some immunocompetent cells, 5099

Palladium(II) complexes – Palladium(II)complexes with R2edda–derived ligands.Part II. Synthesis, characterization and invitro antitumoral studies of R2eddip estersand palladium(II) complexes, 3452

Palladium(II) – Synthesis, spectral studiesand in vitro antibacterial activity ofsteroidal thiosemicarbazone and their palla-dium (Pd (II)) complexes, 2270

PAMAM – Synthesis, characterization andantimicrobial activity of water soluble den-dritic macromolecules, 1093 –Generation–dependent encapsulation/electro-static attachment of phenobarbital moleculesby poly(amidoamine) dendrimers: Evidencefrom 2D–NOESY investigations, 2219

PAMPA – Determination of permeability andlipophilicity of pyrazolo–pyrimidine tyro-sine kinase inhibitors and correlation withbiological data, 3712

Pan agonists – ‘Sum of activities’ as depend-ent parameter: A new CoMFA–basedapproach for the design of pan PPAR ago-nists, 42

Pan PPAR agonists – Important pharma-cophoric features of pan PPAR agonists:Common chemical feature analysis and vir-tual screening, 3488

PAP–1 – 4–Phenoxybutoxy–substituted hete-rocycles – A structure–activity relationshipstudy of blockers of the lymphocyte potas-sium channel Kv1.3, 1838

Paracetamol – Synthesis and pharmacologi-cal evaluation of N–phenyl–acetamide sul-fonamides designed as novel non–hepato-toxic analgesic candidates, 3612

Parallel synthesis – N–Acylated andN,N'–diacylated imidazolidine–2–thionederivatives and N,N'–diacylated tetrahy-dropyrimidine–2(1H)–thione analogues:Synthesis and antiproliferative activity,1106 – Novel modifications in the series ofO–(2–phthalimidoethyl)–N–substitutedthiocarbamates and their ring–opened con-geners as non–nucleoside HIV–1 reversetranscriptase inhibitors, 1650 – Parallel syn-thesis, molecular modelling and furtherstructure–activity relationship studies ofnew acylthiocarbamates as potentnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 2190

Parkinson’s disease – Synthesis of some ureaand thiourea derivatives of3–phenyl/ethyl–2–thioxo–2,3–dihydrothia-zolo[4,5–d]pyrimidine and their antagonisticeffects on haloperidol–induced catalepsy andoxidative stress in mice, 3889 – Facile syn-thesis and in vitro properties of 1–alkyl– and1–alkyl–N–propargyl–1,2,3,4–tetrahydroiso-quinoline derivatives on PC12 cells, 4034

PBS – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

PCAF – Reactivity of isothiazolones andisothiazolone–1–oxides in the inhibition ofthe PCAF histone acetyltransferase, 4855

PEGylation – PEGylated PPI dendritic archi-tectures for sustained delivery of H2 recep-tor antagonist, 1155

Penetratin – Penetratin and derivatives actingas antifungal agents, 212

Penicillin–G – An investigation into the roleof surfactants in controlling particle size ofpolymeric nanocapsules containing peni-cillin–G in double emulsion, 2392

Pentacycloundecane – Pentacyclo–undecanederived cyclic tetra–amines: Synthesis andevaluation as potent anti–tuberculosisagents, 4297

Pentylenetetrazole – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Design, synthesis of 8–alkoxy–5,6–dihy-dro–[1,2,4]triazino[4,3–a]quinolin–1–oneswith anticonvulsant activity, 1265 –Synthesis of novel bioactive derivatives of3–(4–chlorophenyl)–2–hydrazino–5,6,7,8–tetrahydrobenzo(b)thieno[2,3–d]pyrimi-dine–4(3H)–ones, 4721

Pentylenetetrazole test – Synthesis andpotential anticonvulsant activity of new

N–3–substituted 5,5–cyclopropanespirohy-dantoins, 296

Peptide sequenceLys–Hyp–Gly–Glu–Hyp–Ala–Pro–Lys –Circular dichroism studies of type III collagenmimetic peptides with anti– or pro–aggregantactivities on human platelets, 2643

Peptidomimetic – 3D–QSARCoMFA/CoMSIA models based on theoret-ical active conformers ofHOE/BAY–793analogs derived from HIV–1 proteaseinhibitor complexes, 4344

Peptidomimetics – Novel cyclic–imide pep-tidomimetics as aminopeptidase Ninhibitors. Design, chemistry and activityevaluation. Part I, 4819

Peracetic acid oxidation – A macrolactonefrom benzo[a]phenazine with potent activityagainst Mycobacterium tuberculosis, 2334

Perindopril complexes – Molecular structureand stability of perindopril erbumine andperindopril l–arginine complexes, 101

Peripheral benzodiazepine receptor –Synthesis of [11C]FEDAA1106 as a newPET imaging probe of peripheral benzodi-azepine receptor expression, 2748

PET – 11C–labelled PIB analogues as poten-tial tracer agents for in vivo imaging ofamyloid � in Alzheimer’s disease, 1415

PFC – Synthesis, cytotoxicity and effects ofsome 1,2,4–triazole and 1,3,4–thiadiazolederivatives on immunocompetent cells, 63 –Cytotoxicity and effects of 1,10–phenanthro-line and 5–amino–1,10–phenanthroline deriv-atives on some immunocompetent cells, 5099

PGE2 – Synthesis of[1,2,4]triazolo[1,5–a]pyridines of potentialPGE2 inhibitory properties, 1972 – Facilesynthesis of bis(4,5–dihydro–1H–pyra-zole–1–carboxamides) and their thio–ana-logues of potential PGE2 inhibitory proper-ties, 2172

Pharmacodynamic – PEGylated PPI dendrit-ic architectures for sustained delivery of H2receptor antagonist, 1155

Pharmacokinetic – PEGylated PPI dendriticarchitectures for sustained delivery of H2receptor antagonist, 1155

Pharmacokinetics – Synthesis and pharmaco-kinetic evaluation of novel N–acyl–cordy-cepin derivatives with a normal alkyl chain,665 – Didanosine ester prodrugs: Synthesis,albumin binding properties and pharmaco-kinetic studies in rats, 3874

Pharmacological activity – Aziridine alka-loids as potential therapeutic agents, 3373

Pharmacological screening – Analgesic, anti-convulsant and anti–inflammatory activitiesof some synthesized benzodiazipine, tria-zolopyrimidine and bis–imide derivatives,4787

Pharmacophore modeling – Homology mod-eling of MCH1 receptor and validation bydocking/scoring and protein–alignedCoMFA, 2583 – An efficient steroid phar-macophore–based strategy to identify newaromatase inhibitors, 4121 –Pharmacophore modeling and virtualscreening for the discovery of new trans-forming growth factor–� type I receptor(ALK5) inhibitors, 4259

Page 41: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5171

Pharmacophore – Structure–based virtualscreening for identification of novel11�–HSD1 inhibitors, 1167 – Virtual screen-ing for Raf–1 kinase inhibitors based on phar-macophore model of substituted ureas, 1240– A theoretical antioxidant pharmacophorefor resveratrol, 1644 – Fragment and knowl-edge–based design of selective GSK–3�inhibitors using virtual screening models,2361 – 3D–QSAR studies of HDACsinhibitors using pharmacophore–based align-ment, 2868 – Important pharmacophoric fea-tures of pan PPAR agonists: Common chem-ical feature analysis and virtual screening,3488 – Knowledge based identification ofMAO–B selective inhibitors using pharma-cophore and structure based virtual screeningmodels, 3584 – Discovery of potential newInhA direct inhibitors based on pharma-cophoreand 3D–QSAR analysis followed byin silico screening, 3718 – Discovery ofpotential ZAP–70 kinase inhibitors:Pharmacophore design, database screeningand docking studies, 4793

Pharmacophoric model –1,5–Diaryl–2–ethyl pyrrole derivatives asantimycobacterial agents: Design, synthe-sis, and microbiological evaluation, 4734

Phase transfer catalysis – N1–Alkylated3,4–dihydropyrimidine–2(1H)–ones:Convenient one–pot selective synthesis andevaluation of their calcium channel block-ing activity, 1997

Phenanthrenyl phenylalanines – Synthesisof novel N–protected hydrophobic pheny-lalanines and their application in potentialantibacterials, 1001

Phenazines – A macrolactone frombenzo[a]phenazine with potent activityagainst Mycobacterium tuberculosis, 2334

Phenolic compounds – Molecular modelingand inhibition of phospholipase A2 by poly-hydroxy phenolic compounds, 312

Phenothiazine – 10H–Phenothiazines: A newclass of enzyme inhibitors for inflammatorydiseases, 197

Phenothiazines – Synthesis and antimicrobialactivity of some new N–acyl substitutedphenothiazines, 5094

Phenylbenzoimidazole – Synthesis and affin-ity to DNA of phenylbenzoimidazoles andbenzoimidazo[1,2–c]quinazolines, 3305

Phenylbenzothiazole – 11C–labelled PIB ana-logues as potential tracer agents for in vivoimaging of amyloid � in Alzheimer’s dis-ease, 1415

Phenylpyrrole derivatives – Phenylpyrrolederivatives as neural and inducible nitricoxide synthase (nNOS and iNOS)inhibitors, 2655

BPH–027 – Synthesis and antibacterial activity

of novel 5–(4–methyl–1H–1,2,3–triazole)methyl oxazolidinones, 3217

PPhonate metal complexes – Some

O,O',O",O–di/tetra aryldithioimi-dophonate transition metal complexes

derived from catechol and bisphenol–A asantibacterial and antifungal agents, 785

Phosphole–and phosphonate derivatives –Application of phosphonyl carbanions tohighly regioselective synthesis of somediazaphospholes and pyrazolinyl phospho-nates, 526

Phosphoramidates – The novel phospho-ramidate derivatives of NSAID 3–hydrox-ypropylamides: Synthesis, cytostatic andantiviral activity evaluations, 143

Phosphorus heterocycles – Synthesis andantibacterial activity of some new thiadi-a z a / t r i a z a p h o s p h o l e s ,thiadiaza/triaza/tetrazaphosphinines andthiadiaza/tetrazaphosphepines containing1,2,4–triazinone moiety, 4539

Photobiological activity – Tetrahydrobenzo–and benzofurobenzopyrones as a new classof potential photoreagents toward DNA, 18

Photochemistry – Synthesis and cytotoxicactivity of �–santonin derivatives, 3739

Photochemotherapeutic agents –Tetrahydrobenzo– and benzofurobenzopy-rones as a new class of potential photore-agents toward DNA, 18

Photocleavage – Synthesis and DNA–bindingstudies of two ruthenium(II) complexes ofan intercalating ligand, 2044

Photodynamic inactivation – Photodynamicinactivation of Candida albicans sensitizedby tri– and tetra–cationic porphyrin deriva-tives, 1592

Photogenotoxicity – Photo–inducible cyto-toxic and clastogenic activities of3,6–di–substituted acridines obtained byacylation of proflavine, 2459

Photoisomerization – Synthesis, photochem-ical E (trans)�Z (cis) isomerization andantimicrobial activity of 2–chloro–5–methylpyridine–3–olefin derivatives, 4661

Photosensitizers – Photodynamic inactivationof Candida albicans sensitized by tri– andtetra–cationic porphyrin derivatives, 1592

Phototoxicity – Photo–inducible cytotoxicand clastogenic activities of 3,6–di–substi-tuted acridines obtained by acylation ofproflavine, 2459

Phthalazine – Synthesis and antibacterialactivity of some new heterocycles incorpo-rating phthalazine, 4448

Phthalimide – Synthesis and antimicrobialactivity of some new N–acyl substitutedphenothiazines, 5094

Physicochemical – Physicochemical and bio-logical characterization of novel macrocy-cles derived from o–phthalaldehyde, 2621

Physico–chemical property – Determinationof permeability and lipophilicity of pyrazo-lo–pyrimidine tyrosine kinase inhibitors andcorrelation with biological data, 3712

PIB – 11C–labelled PIB analogues as potentialtracer agents for in vivo imaging of amyloid� in Alzheimer’s disease, 1415

Pictet–Spengler cyclization – Design, syn-thesis and biological evaluation of novelnitrogen and sulfur containinghetero–1,4–naphthoquinones as potent anti-fungal and antibacterial agents, 3130

Pictet–Spengler reaction – Facile synthesisand in vitro properties of 1–alkyl– and

1–alkyl–N–propargyl–1,2,3,4–tetrahy-droisoquinoline derivatives on PC12 cells,4034

Piperazine – Synthesis and antimalarial activ-ity of hydroxyethylpiperazine derivatives,1363

Piperidine – Evaluation of in vivowound–healing potential of2–[4–(2,4–dimethoxy–benzoyl)–phe-noxy]–1–[4–(3–piperidin–4–yl–propyl)–piperidin–1–yl]–ethanone derivatives, 3158

Piperidin–4–one – Synthesis and spectralcharacterization of a new class ofN–(N–methylpiperazinoacetyl)–2,6–diarylpiperidin–4–ones: Antimicrobial, analgesicand antipyretic studies, 577

Piperine analogs – Quantitative structureactivity relationship (QSAR) of piperineanalogsfor bacterial NorA efflux pumpinhibitors, 4128

Piroxicam – Synthesis and structure analysisof cyclodehydration product of piroxicam:A metabolite detected in dogs and monkeys,3368

PLA2 – Molecular modeling and inhibition ofphospholipase A2 by polyhydroxy phenoliccompounds, 312

Plants – Aziridine alkaloids as potential thera-peutic agents, 3373

Plasma – Highly sensitive spectrofluorimetricdetermination of lomefloxacin in spikedhuman plasma, urine and pharmaceuticalpreparations, 3402

Plasma protein binding – Prediction of vol-ume of distribution values in human usingimmobilized artificial membrane partition-ing coefficients, the fraction of compoundionized and plasma protein binding data,4455

Plasmid DNA – Synthesis and characteriza-tion of dinuclear macrocyclic cobalt(II),copper(II) and zinc(II) complexes derivedfrom 2,2,2',2'–S,S[bis(bis–N,N–2–thiobenz-imidazolyloxalato–1,2–ethane)]: DNAbinding and cleavage studies, 834

Plasmid Supercoil relaxation assays –Synthesis and biological activity evaluationof 1H–benzimidazoles via mammalianDNA topoisomerase I and cytostaticityassays, 2280

Plasmodium berghei – Synthesis and anti-malarial activity of pyrazolo and pyrimidobenzothiazine dioxide derivatives, 1303

Plasmodium falciparum – Antiplasmodialand antitrypanosomal activities of aminobi-cyclo[2.2.2]octyl �–aminoalkanoates, 736– New antimalarial and cytotoxic4–nerolidylcatechol derivatives, 2731 –Design and in silico screening of combina-torial library of antimalarial analogs of tri-closan inhibiting Plasmodium falciparumenoyl–acyl carrier protein reductase, 3009 –Search for new pharmacophores for anti-malarial activity. Part III: Synthesis and bio-evaluation of new 6–thioureido–4–anilino-quinazolines, 4404 – Synthesis and anti-malarial activity of new atovaquone deriva-tives, 4778 – A new series of amodiaquineanalogues modified in the basic side chainwith in vitro antileishmanial and antiplas-modial activity, 5071

Page 42: Chal Micro

5172 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Plasmodium – Primaquine revisited sixdecades after its discovery, 937

Platinum complex – Synthesis and antituber-cular activity of palladium and platinumcomplexes with fluoroquinolones, 4107

Platinum – Synthesis, characterisation and invitro cytotoxicity studies of a series of chi-ral platinum(II) complexes based on the2–aminomethylpyrrolidine ligand: X–raycrystal structure of [PtCl2(R–dimepyrr)](R–dimepyrr=N–dimethyl–2(R)–aminomethylpyrrolidine), 2807

Platinum(II) complexes – Cytotoxic activityand chemical reactivity of cis–platinum(II)and trans–palladium(II) complexes withdiethyl (pyridinylmethyl)phosphates, 660

Platinum(II) complexes – In vitro and in vivoantitumor activity of platinum(II) complex-es with thiosemicarbazones derived from2–formyl and 2–acetyl pyridine and con-taining ring incorporated at N(4)–position:Synthesis, spectroscopic study and crystalstructure of platinum(II) complexes withthiosemicarbazones, potential anticanceragents, 1296

Platinum(II) – Novel trans–dichloridoplat-inum(II) complexes with 3– and4–acetylpyridine: Synthesis, characteriza-tion, DFT calculations and cytotoxicity,1921

PLS – A set of new amino acid descriptorsapplied in prediction of MHC class I bind-ing peptides, 1144 – QSAR model for pre-dicting radical scavenging activity of di(het-ero)arylamines derivatives of benzo[b]thio-phenes, 1952 – Juglone derivatives as anti-tubercular agents: A rationale for the activi-ty profile, 2847 – Comparative chemomet-ric modeling of cytochrome 3A4 inhibitoryactivity of structurally diverse compoundsusing stepwise MLR, FA–MLR, PLS, GFA,G/PLS and ANN techniques, 2913 –Multivariate QSAR study of 4,5–dihydrox-ypyrimidine carboxamides as HIV–1 inte-grase inhibitors, 3577

Polar surface area – Anti–nitric oxide pro-duction activity of isothiocyanates corre-lates with their polar surface area rather thantheir lipophilicity, 4931

Pollutants – Prediction of milk/plasma con-centration ratios of drugs and environmentalpollutants, 2452

Polyamidoamine – Generation–dependentencapsulation/electrostatic attachment ofphenobarbital molecules by poly(ami-doamine) dendrimers: Evidence from2D–NOESY investigations, 2219

Polyamine conjugate – Synthesis, cytotoxicityand apoptosis of naphthalimide polyamineconjugates as antitumor agents, 393

Polyamines – Oligonucleotide–polyamineconjugates: Influence of length and positionof 2'–attached polyamines on duplex stabil-ity and antisense effect, 670 – Preparationof spermine conjugates with acidic retinoidswith potent ribonuclease P inhibitory activi-ty, 2689

Polybutyl adipate – An investigation into therole of surfactants in controlling particlesize of polymeric nanocapsules containingpenicillin–G in double emulsion, 2392

Polycyclic cage – Polycyclic cage structuresas carrier molecules for neuroprotectivenon–steroidal anti–inflammatory drugs,2577

Polydentate nitrogen ligands – Synthetic,structural and biochemical studies ofpolynuclear platinum(II) complexes withheterocyclic ligands, 1041

Polymer–bound reagents – Synthesis of aseries of N6–substituted adenosines withactivity against trypanosomatid parasites,3665

Polymer–metal complex – DNA binding andantimicrobial studies of polymer–copper(II)complexes containing 1,10–phenanthrolineand l–phenylalanine ligands, 1878

Polynuclear platinum complexes –Synthetic, structural and biochemical stud-ies of polynuclear platinum(II) complexeswith heterocyclic ligands, 1041

Polyphenols – QSAR study of antioxidantactivity of wine polyphenols, 400

Polypyridyl – Synthesis and DNA–bindingstudies of two ruthenium(II) complexes ofan intercalating ligand, 2044

Porphyrin–fullerenes – Theporphyrin–fullerene nanoparticles to pro-mote the ATP overproduction in myocardi-um: 25Mg2�–magnetic isotope effect, 1554

Positive inotropic activity – Synthesis of2–(4–substitutedmethylpiperazin–1–yl)–N–(3,4–dihydro–3–oxo–2H–benzo[b][1,4]oxazin–7–yl)acetamides and their positiveinotropic evaluation, 3027

Positron emission tomography – Analogs ofJHU75528, a PET ligand for imaging ofcerebral cannabinoid receptors (CB1):Development of ligands with optimizedlipophilicity and binding affinity, 593 –Simple synthesis of carbon–11 labeledstyryl dyes as new potential PET RNA–spe-cific, living cell imaging probes, 2300 –Synthesis of [11C]FEDAA1106 as a newPET imaging probe of peripheral benzodi-azepine receptor expression, 2748

Potassium channel openers – QSAR model-ling of pancreatic �–cell KATP channelopeners R/S–3,4–dihydro–2,2–dimethyl–6–halo–4–(substituted pheny-laminocarbonylamino)–2H–1–benzopyransusing MLR–FA techniques, 359

Potential antitumor agents – Novel8–deaza–5,6,7,8–tetrahydroaminopterinderivatives as dihydrofolate inhibitor:Design, synthesis and antifolate activity,764

Potential inhibitors – Diacylhydrazine deriv-atives as novel potential chitin biosynthesisinhibitors: Design, synthesis, and struc-ture–activity relationship, 2985

Potential of mean force – Potential of meanforce for Syrian hamster prion epitope pro-tein – Monoclonal fab 3f4 antibody interac-tion studies, 3504

Potentiators – Quantitative structure–activityrelationship (QSAR) of aryl alkenylamides/imines for bacterial efflux pumpinhibitors, 229 – Quantitative structureactivity relationship (QSAR) of piperineanalogsfor bacterial NorA efflux pumpinhibitors, 4128

Poxviruses – Synthesis and antiviral activityof new pyrazole and thiazole derivatives,3746

PPA cyclization – Synthesis, analgesic,anti–inflammatory and antimicrobial stud-ies of 2,4–dichloro–5–fluorophenyl con-taining thiazolotriazoles, 827

PPAR – ‘Sum of activities’ as dependentparameter: A new CoMFA–based approachfor the design of pan PPAR agonists, 42

PPI dendrimers – PEGylated PPI dendriticarchitectures for sustained delivery of H2receptor antagonist, 1155

PPR – Prediction of CCR5 receptor bindingaffinity of substituted 1–(3,3–diphenyl-propyl)–piperidinyl amides and ureas basedon the heuristic method, support vectormachine and projection pursuit regression,25 – QSAR models for 2–amino–6–arylsul-fonylbenzonitriles and congeners HIV–1reverse transcriptase inhibitors based on lin-ear and nonlinear regression methods, 2158

Prasterone – To determine the cytotoxicity ofchlorambucil and one of its nitro–deriva-tives, conjugated to prasterone and preg-nenolone, towards eight human cancercell–lines, 2944

Prato reaction – Fullerene derivatized s–tri-azine analogues as antimicrobial agents,2178

pRb – Synthesis and antiproliferative activityof 3–amino–N–phenyl–1H–indazole–1–carboxamides, 165

Pregnenolone – To determine the cytotoxicityof chlorambucil and one of its nitro–deriva-tives, conjugated to prasterone and preg-nenolone, towards eight human cancercell–lines, 2944

Prenyl – Synthesis of (±)Abyssinone I andrelated compounds: Their anti–oxidant andcytotoxic activities, 2239

Preservatives – Preparation and antimicrobialbehaviour of quaternary ammonium thiolderivatives able to be grafted on metal sur-faces, 717 – Enhanced activity of fluorinat-ed quaternary ammonium surfactantsagainst Pseudomonas aeruginosa, 1615 –Synthesis and antimicrobial properties ofpolymerizable quaternary ammoniums,3201 – Contact–active microbicidal goldsurfaces using immobilization of quaternaryammonium thiol derivatives, 4227

Primaquine – Primaquine revisited sixdecades after its discovery, 937 –Primaquine dipeptide derivatives bearing animidazolidin–4–one moiety at the N–termi-nus as potential antimalarial prodrugs, 2506

Principal component analysis – New poten-tial AChE inhibitor candidates, 3754

Prion – Potential of mean force for Syrianhamster prion epitope protein – Monoclonalfab 3f4 antibody interaction studies, 3504

Prodrug – Novel derivatives of 6–mercaptop-urine: Synthesis, characterization andantiproliferative activities ofS–allylthio–mercaptopurines, 541 –Towards an efficient prodrug of the alkylat-ing metabolite monomethyltriazene:Synthesis and stability of N–acylamino acidderivatives of triazenes, 1049 –Structure–activity relationships for dipep-

Page 43: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5173

tide prodrugs of acyclovir: Implications forprodrug design, 2339

Prodrugs – Primaquine dipeptide derivativesbearing an imidazolidin–4–one moiety atthe N–terminus as potential antimalarialprodrugs, 2506 – Polycyclic cage structuresas carrier molecules for neuroprotectivenon–steroidal anti–inflammatory drugs,2577 – Dopamine– and tyramine–basedderivatives of triazenes: Activation bytyrosinase and implications for prodrugdesign, 3228 – Didanosine ester prodrugs:Synthesis, albumin binding properties andpharmacokinetic studies in rats, 3874

Proflavine derivatives – Photo–induciblecytotoxic and clastogenic activities of3,6–di–substituted acridines obtained byacylation of proflavine, 2459

Prolinamides – The influence of an ethylenespacer on the 5–HT1A and 5–HT2A receptoraffinity of arylpiperazine derivatives ofamides with N–acylated amino acids and3–differently substitutedpyrrolidine–2,5–diones, 800

Promastigote – Synthesis, biological evalua-tion and SAR of sulfonamide 4–methoxy-chalcone derivatives with potentialantileishmanial activity, 755

Pro–cognitive agents – Diamine–basedhuman histamine H3 receptor antagonists:(4–Aminobutyn–1–yl)benzylamines, 4098

Propanehydrazonoyl chlorides –Stereoselective synthesis and antimicrobialactivity of benzofuran–based(1E)–1–(piperidin–1–yl)–N2–arylamidra-zones, 4985

Propargyl group – Facile synthesis and invitro properties of 1–alkyl– and1–alkyl–N–propargyl–1,2,3,4–tetrahy-droisoquinoline derivatives on PC12 cells,4034

Prostaglandin synthetase –10H–Phenothiazines: A new class ofenzyme inhibitors for inflammatory dis-eases, 197

Prostate cancer cells – Effect of conjugates ofall–trans–retinoic acid and shorter polyenechain analogues with amino acids onprostate cancer cell growth, 3175

Prostate cancer – Novel CYP17 inhibitors:Synthesis, biological evaluation,structure–activity relationships and model-ling of methoxy– and hydroxy–substitutedmethyleneimidazolyl biphenyls, 2765

Protease inhibitor – Synthesis, antimalarialevaluation and molecular modeling studiesof hydroxyethylpiperazines, potentialaspartyl protease inhibitors, Part 2, 3816

Protease M14 family – A new type offive–membered heterocyclic inhibitors ofbasic metallocarboxypeptidases, 3266

Proteases – Natural polyprenylated benzophe-nones inhibiting cysteine and serine pro-teases, 1230

Proteasome inhibition – Metals in anticancertherapy: Copper(II) complexes as inhibitorsof the 20S proteasome, 4353

Proteasome inhibitors – 3D–QSAR studiesof boron–containing dipeptides as protea-some inhibitors with CoMFA and CoMSIAmethods, 1486

Protein binding – Didanosine ester prodrugs:Synthesis, albumin binding properties andpharmacokinetic studies in rats, 3874

Protein kinase inhibitors – Design, synthesisand characterization of N9/N7–substituted6–aminopurines as VEGF–R and EGF–Rinhibitors, 1788

Protein synthesis – Antifungal unsaturatedcyclic Mannich ketones and amino alco-hols: Study of mechanism of action, 1823

Protein tyrosine phoshatase–1B inhibitors –Novel 2–aryl–naphtho[1,2–d]oxazole deriv-atives as potential PTP–1B inhibitors show-ing antihyperglycemic activities, 109

Protein tyrosine phosphatase 1B, PTP1B –Structure–based virtual screening approachto identify novel classes of PTP1Binhibitors, 3280

Pseudohypha – Antifungal unsaturated cyclicMannich ketones and amino alcohols: Studyof mechanism of action, 1823

Pseudomonas aeruginosa – Enhanced activityof fluorinated quaternary ammonium surfac-tants against Pseudomonas aeruginosa, 1615

Pterocarpans –(±)–3,4–Dihydroxy–8,9–methylene-dioxypterocarpan and derivatives:Cytotoxic effect on human leukemia celllines, 920

PTP1B inhibition – Synthesis and evaluationof some novel isochroman carboxylic acidderivatives as potential anti–diabetic agents,3147

Pyrazine – Synthesis and antimycobacterialactivity of N'–[(E)–(monosubstituted–ben-zylidene)]–2–pyrazinecarbohydrazidederivatives, 4954

Pyrazol – Synthesis and antimalarial activityof pyrazolo and pyrimido benzothiazinedioxide derivatives, 1303

Pyrazole – Synthesis and molluscicidal activ-ity of some new thiophene, thiadiazole andpyrazole derivatives, 1250 – Synthesis ofnovel pyrazole derivatives and evaluation oftheir antidepressant and anticonvulsantactivities, 3480 – Synthesis and antiviralactivity of new pyrazole and thiazole deriv-atives, 3746 – Antioxidant and antibacterialstudies of arylazopyrazoles and arylhydra-zonopyrazolones containing coumarin moi-ety, 4690

Pyrazoles – Synthesis and anti–HSV–1 evalu-ation of some pyrazoles and fused pyra-zolopyrimidines, 3285 – Convenient syn-thesis and antimicrobial evaluation of somenovel 2–substituted–3–methylbenzofuranderivatives, 3637

Pyrazoline – Synthesis and pharmacologicalevaluation of a novel series of 5–(substitut-ed)aryl–3–(3–coumarinyl)–1–phenyl–2–pyrazolines as novel anti–inflammatory andanalgesic agents, 1682 – Synthesis andantinociceptive activities of some pyrazo-line derivatives, 2606

Pyrazolines – Synthesis, spectral studies andantiamoebic activity of new 1–N–substitut-ed thiocarbamoyl–3–phenyl–2–pyrazolines,417 – Synthesis of novel thiazolone–basedcompounds containing pyrazoline moietyand evaluation of their anticancer activity,1396

Pyrazolo[3,4–b]pyridines – Synthesis ofsome novel pyrazolo[3,4–b]pyridine andpyrazolo[3,4–d]pyrimidine derivativesbearing 5,6–diphenyl–1,2,4–triazine moietyas potential antimicrobial agents, 4385

Pyrazolo[3,4–d]pyrimidines – Synthesis ofsome novel pyrazolo[3,4–b]pyridine andpyrazolo[3,4–d]pyrimidine derivativesbearing 5,6–diphenyl–1,2,4–triazine moietyas potential antimicrobial agents, 4385

Pyrazolo[4,3–e][1,2,4]triazines –Cyclocondensation reaction of heterocycliccarbonyl compounds, Part XIII: Synthesisand cytotoxic activity of some3,7–diaryl–5–(3,4,5–trimethoxyphenyl)pyrazolo[4,3–e][1,2,4]triazines, 891

Pyrazolopyridine – New pyridone, thioxopy-ridine, pyrazolopyridine and pyridine deriv-atives that modulate inflammatory media-tors in stimulated RAW 264.7 murinemacrophage, 4547

Pyrazolopyrimidines – Synthesis andanti–HSV–1 evaluation of some pyrazolesand fused pyrazolopyrimidines, 3285

Pyridazine – Novel pyridazine derivatives:Synthesis and antimicrobial activity evalua-tion, 1989

Pyridazinone – Synthesis and blood glucoselowering effect of novel pyridazinone sub-stituted benzenesulfonylurea derivatives,2673 – Synthesis and analgesic andanti–inflammatory activities 6–substitut-ed–3(2H)–pyridazinone–2–acetyl–2–(p–substituted/nonsubstituted benzal)hydrazonederivatives, 3760

Pyridazinones – Synthesis and vasodilatoryactivity of some amide derivatives of6–(4–carboxymethyloxyphenyl)–4,5–dihy-dro–3(2H)–pyridazinone, 4441

Pyridine derivatives – Cytotoxic activity andchemical reactivity of cis–platinum(II) andtrans–palladium(II) complexes with diethyl(pyridinylmethyl)phosphates, 660

Pyridine estrogen – Phenethyl pyridines withnon–polar internal substitutents as selectiveligands for estrogen receptor beta, 3560

Pyridine – Copper complexes of pyridinederivatives with superoxide scavenging andantimicrobial activities, 3259 – New pyri-done, thioxopyridine, pyrazolopyridine andpyridine derivatives that modulate inflam-matory mediators in stimulated RAW 264.7murine macrophage, 4547

Pyrido[1,2–a]pyrimidines – Synthesis andevaluation of pyrido[1,2–a]pyrimidines asinhibitors of nitric oxide synthases, 2877

Pyrido[1,2–c]pyrimidines – Novel4–aryl–pyrido[1,2–c]pyrimidines with dualSSRI and 5–HT1A activity, Part 1, 1710

Pyrido[1,2–c]pyrimidines – Novel4–aryl–pyrido[1,2–c]pyrimidines with dualSSRI and 5–HT1A activity: Part 2, 4702

Pyrido[2,3–d]pyrimidines – Synthesis ofnew 2–substituted pyrido[2,3–d]pyrim-idin–4(1H)–ones and their antibacterialactivity, 1369

Pyridocarbazoles – Photochemical electrocy-clisation of 3–vinylindoles to pyrido[2,3–a]–,pyrido[4,3–a]– and thieno[2,3–a]–car-bazoles: Design, synthesis, DNA binding andantitumor cell cytotoxicity, 3235

Page 44: Chal Micro

5174 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Pyridone – New pyridone, thioxopyridine,pyrazolopyridine and pyridine derivativesthat modulate inflammatory mediators instimulated RAW 264.7 murine macrophage,4547

Pyrimidine – Synthesis and antimalarialactivity of pyrazolo and pyrimido benzoth-iazine dioxide derivatives, 1303 – Acyclicnucleoside bisphosphonates: Synthesis andproperties of chiral 2–amino–4,6–bis[(phos-phonomethoxy)alkoxy]pyrimidines, 2408 –Synthesis and antileishmanial activity ofnovel 2,4,6–trisubstituted pyrimidines and1,3,5–triazines, 2473

Pyrimidines – Synthesis of new 2–substitutedpyrido[2,3–d]pyrimidin–4(1H)–ones andtheir antibacterial activity, 1369 –Substituted quinolinyl chalcones and quino-linyl pyrimidines as a new class ofanti–infective agents, 2081 –Enaminonitrile in heterocyclic synthesis:Synthesis and antimicrobial evaluation ofsome new pyrazole, isoxazole and pyrimi-dine derivatives incorporating a benzothia-zole moiety, 4813

Pyrimido[4,5–b]quinolone – Design and syn-thesis of azolopyrimidoquinolines, pyrimi-doquinazolines as anti–oxidant,anti–inflammatory and analgesic activities,609

Pyrroles – Synthesis and bioassay of a newclass of heterocycles pyrrolyloxadiazoles/thiadiazoles/triazoles, 2313

Pyrrolidine carboxamide – Discovery ofpotential new InhA direct inhibitors basedon pharmacophoreand 3D–QSAR analysisfollowed by in silico screening, 3718

Pyrrolidine–2,5–dione – The influence of anethylene spacer on the 5–HT1A and 5–HT2Areceptor affinity of arylpiperazine deriva-tives of amides with N–acylated aminoacids and 3–differently substituted pyrroli-dine–2,5–diones, 800

Pyrrolidine–5–one–carboxamide – Theinfluence of an ethylene spacer on the5–HT1A and 5–HT2A receptor affinity ofarylpiperazine derivatives of amides withN–acylated amino acids and 3–differentlysubstituted pyrrolidine–2,5–diones, 800

Pyrrolo[1,2–c]pyrimidines – Synthesis, anal-gesic and anti–inflammatory activities eval-uation of some bi–, tri– and tetracyclic con-densed pyrimidines, 4572

Pyrroloquinoline – DNA–targeting pyrrolo-quinoline–linked butenone and chalcones:Synthesis and biological evaluation, 2854

QQAAR – Exploring QSAR and QAAR for

inhibitors of cytochrome P450 2A6 and2A5 enzymes using GFA and G/PLS tech-niques, 1941

QSAR modelling – QSAR modelling of pan-creatic �–cell KATP channel openersR/S–3,4–dihydro–2,2–dimethyl–6–halo–4–( s u b s t i t u t e dphenylaminocarbonylamino)–2H–1–ben-zopyrans using MLR–FA techniques, 359

QSAR – Prediction of CCR5 receptor bindingaffinity of substituted 1–(3,3–diphenyl-

propyl)–piperidinyl amides and ureas basedon the heuristic method, support vectormachine and projection pursuit regression,25 – ‘Sum of activities’ as dependentparameter: A new CoMFA–based approachfor the design of pan PPAR agonists, 42 –Possible anticancer agents: QSAR analogsof glutamamide: Synthesis and pharmaco-logical activity of 1,5–N,N'–disubstitut-ed–2–(substituted benzenesulphonyl) gluta-mamides, 70 – Quantitative structure–activ-ity relationship (QSAR) of aryl alkenylamides/imines for bacterial efflux pumpinhibitors, 229 – Larvicidal activities ofsome organotin compounds on mosquitolarvae: A QSAR study, 260 –Antileukotrienic phenethylamido deriva-tives of arylalkanoic acids in the treatmentof ulcerative colitis, 332 – QSAR study ofantioxidant activity of wine polyphenols,400 – Evaluation of the local anaestheticactivity of 3–aminobenzo[d]isothiazolederivatives using the rat sciatic nervemodel, 473 – Hansch analysis of veratricacid derivatives as antimicrobial agents, 689– QSAR analysis of salicylamide isostereswith the use of quantum chemical moleculardescriptors, 869 – A novel QSAR model forpredicting the inhibition of CXCR3 receptorby 4–N–aryl–[1,4] diazepane ureas, 877 –Synthesis and QSAR evaluation of 2–(sub-stituted phenyl)–1H–benzimidazoles and[ 2 – ( s u b s t i t u t e dphenyl)–benzimidazol–1–yl]–pyridin–3–yl–methanones, 1119 – A set of new aminoacid descriptors applied in prediction ofMHC class I binding peptides, 1144 –Predictive QSAR modeling of HIV reversetranscriptase inhibitor TIBO derivatives,1509 – Design, synthesis, structure–activityrelationship and antibacterial activity seriesof novel imidazo fused quinolone carbox-amides, 1570 – Modeling the activity offurin inhibitors using artificial neural net-work, 1664 – Antifungal unsaturated cyclicMannich ketones and amino alcohols: Studyof mechanism of action, 1823 – Hanschanalysis of substituted benzoic acid benzyli-dene/furan–2–yl–methylene hydrazides asantimicrobial agents, 1853 – ExploringQSAR and QAAR for inhibitors ofcytochrome P450 2A6 and 2A5 enzymesusing GFA and G/PLS techniques, 1941 –QSAR model for predicting radical scav-enging activity of di(hetero)arylaminesderivatives of benzo[b]thiophenes, 1952 –Synthesis, antimicrobial evaluation andQSAR study of some 3–hydroxypyri-dine–4–one and 3–hydroxypyran–4–onederivatives, 2145 – QSAR models for2–amino–6–arylsulfonylbenzonitriles andcongeners HIV–1 reverse transcriptaseinhibitors based on linear and nonlinearregression methods, 2158 – CoMFA anddocking studies of 2–phenylindole deriva-tives with anticancer activity, 2822 –Comparative chemometric modeling ofcytochrome 3A4 inhibitory activity of struc-turally diverse compounds using stepwiseMLR, FA–MLR, PLS, GFA, G/PLS andANN techniques, 2913 – Diacylhydrazine

derivatives as novel potential chitin biosyn-thesis inhibitors: Design, synthesis, andstructure–activity relationship, 2985 –Multivariate QSAR study of 4,5–dihydrox-ypyrimidine carboxamides as HIV–1 inte-grase inhibitors, 3577 – QSAR study ofAkt/protein kinase B (PKB) inhibitors usingsupport vector machine, 4090 –Quantitative structure activity relationship(QSAR) of piperine analogsfor bacterialNorA efflux pump inhibitors, 4128 –Scoring function for DNA–drug docking ofanticancer and antiparasitic compoundsbased on spectral moments of 2D latticegraphsfor molecular dynamics trajectories,4461 – Multi–target spectral moments forQSAR and Complex Networks study ofantibacterial drugs, 4516 – Prediction oftelomerase inhibitory activity for acridinicderivatives based on chemical structure,4826 – Application of geneticalgorithm–support vector machine(GA–SVM) for prediction of BK–channelsactivity, 5023

QSAR study – Juglone derivatives as antitu-bercular agents: A rationale for the activityprofile, 2847

QSPR – QSPR modeling bioconcentrationfactor (BCF) by balance of correlations,2544

Quantitative structure–activity relationship(QSAR) – A QSAR study for the cytotoxicactivities of taxoids against macrophage(M)–like cells, 274

Quantitative structure–activity relationship(QSAR) – Quantitative structure–activityrelationship analysis of aryl alkanol piper-azine derivatives with antidepressant activi-ties, 4367 – Synthesis and QSAR modelingof 2–acetyl–2–ethoxycarbonyl–1–[4(4'–ary-lazo)–phenyl]–N,N–dimethylaminophenylaziridines as potential antibacterial agents,251 – Topological descriptors in modelingthe agonistic activity of human A3 adeno-sine receptor ligands: The derivatives of2–chloro–N6–substituted–4'–thioadeno-sine–5'–uronamide, 1377

Quantitative structure–activity relationship– Quantitative structure–activity relation-ship study of serotonin (5–HT7) receptorinhibitors using modified ant colony algo-rithm and adaptive neuro–fuzzy interfer-ence system (ANFIS), 1463 – Preparationand in vitro evaluation of benzylsulfanylbenzoxazole derivatives as potential antitu-berculosis agents, 2286 – Development ofQSAR models for predicting hepatocarcino-genic toxicity of chemicals, 3658 –Predicting the activity of drugs for a groupof imidazopyridine anticoccidial com-pounds, 4044

Quantum chemical calculations – Synthesis,pharmacological screening, quantum chem-ical and in vitro permeability studies ofN–Mannich bases of benzimidazolesthrough bovine cornea, 2307

Quaternary ammonium compounds –Synthesis and antimicrobial properties ofpolymerizable quaternary ammoniums,3201 – Dialkylamino and nitrogen hetero-cyclic analogues of hexadecylphospho-

Page 45: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5175

choline and cetyltrimetylammonium bro-mide: Effect of phosphate group and envi-ronment of the ammonium cation on theirbiological activity, 4970

Quaternary ammonium salts – Preparationand antimicrobial behaviour of quaternaryammonium thiol derivatives able to begrafted on metal surfaces, 717 – Enhancedactivity of fluorinated quaternary ammoni-um surfactants against Pseudomonas aerug-inosa, 1615 – Novel topoisomerase I–tar-geting antitumor agents synthesized fromthe N,N,N–trimethylammonium derivativeof ARC–111,5H–2,3–dimethoxy–8,9–methylene-dioxy–5–[(2–N,N,N–trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin–6–oneiodide, 3433 – Contact–active microbicidalgold surfaces using immobilization of qua-ternary ammonium thiol derivatives, 4227

Quercetin – Discovering novelquercetin–3–O–amino acid–esters as a newclass of Src tyrosine kinase inhibitors, 1982

Quinazoline – Search for new pharma-cophores for antimalarial activity. Part III:Synthesis and bioevaluation of new6–thioureido–4–anilinoquinazolines, 4404

Quinazolines – Promising carboranylquinazo-lines for boron neutron capture therapy:Synthesis, characterization, and in vitro tox-icity evaluation, 409

Quinazolin–4(3H)–one – Synthesis andanti–microbial screening of some Schiffbases of 3–amino–6,8–dibromo–2–phenylquinazolin–4(3H)–ones, 2328

Quinazolin–4–ones – Synthesis andanti–inflammatory activity of newer quina-zolin–4–one derivatives, 83

Quinazolinone – Antimicrobial studies ofsome novel quinazolinones fused with[1,2,4]–triazole, [1,2,4]–triazine and[1,2,4,5]–tetrazine rings, 1188

Quinoline – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Design, synthesis and anticancer evalua-tion of novel tetrahydroquinoline deriva-tives containing sulfonamide moiety, 4211 –Synthesis and antimicrobial activities ofnovel quinoline derivatives carrying1,2,4–triazole moiety, 4637

Quinolines – Design, synthesis,structure–activity relationship and antibac-terial activity series of novel imidazo fusedquinolone carboxamides, 1570 – Synthesisand antimycobacterial activities of novel6–nitroquinolone–3–carboxylic acids, 345 –Synthesis and antibacterial activity ofnitroaryl thiadiazole–gatifloxacin hybrids,1205

Quinones – (±)–3,4–Dihydroxy–8,9–methyl-enedioxypterocarpan and derivatives:Cytotoxic effect on human leukemia celllines, 920

Quinoxaline – Synthesis of some new 4–styryl-tetrazolo[1,5–a]quinoxaline and 1–substitut-ed–4–styryl[1,2,4]triazolo[4,3–a]quinoxalinederivatives as potent anticonvulsants, 1135

Quorum sensing – Synthesis and evaluationof antibacterial activities of andro-grapholide analogues, 2936

RRadical scavenging – Synthesis of

(±)Abyssinone I and related compounds:Their anti–oxidant and cytotoxic activities,2239

Radioligand binding assays – Substitutedbenzo[d]oxazol–2(3H)–one derivativeswith preference for the �1 binding site, 124– Synthesis of a series of8–(substituted–phenyl)xanthines and astudy on the effects of substitution patternof phenyl substituents on affinity for adeno-sine A1 and A2A receptors, 2122

Raf–1 kinase inhibitors – Virtual screeningfor Raf–1 kinase inhibitors based on phar-macophore model of substituted ureas, 1240

Raman – Synthesis, Raman, FT–IR, NMRspectroscopic data and antimicrobial activi-ty of mixed aza–oxo–thia macrocyclic com-pounds, 365

Random forest – Classification models forCYP450 3A4 inhibitors and non–inhibitors,2354

Rare earths – Crystal structures, antioxida-tion and DNA binding properties of Dy(III)complexes with Schiff–base ligands derivedfrom 8–hydroxyquinoline–2–carboxalde-hyde and four aroylhydrazines, 5080

Rational design – On designing non–saccha-ride, allosteric activators of antithrombin,2626 – New azoles with potent antifungalactivity: Design, synthesis and moleculardocking, 4218

RCM reaction – Large ring 1,3–bridged2–azetidinones: Experimental and theoreti-cal studies, 2071

Reactivators – In–vitro regeneration of sarininhibited electric eel acetylcholinesterase bybis–pyridinium oximes bearing xylene link-er, 1326 – Synthesis and evaluation of novelbis–pyridinium oximes as reactivators ofDFP–inhibited acetylcholinesterase, 1335

Real time fluorescence microscopy –Unusual cellular uptake of cytotoxic4–hydroxymethyl–3–aminoacridine, 4758

Rebeccamycin – A three–step synthesis fromrebeccamycin of an efficient checkpointkinase 1 inhibitor, 2234

Receptor binding studies – Synthesis of �receptor ligands with unsymmetrical spiroconnection of the piperidine moiety, 4306

Receptor docking – Analogs of JHU75528, aPET ligand for imaging of cerebral cannabi-noid receptors (CB1): Development of lig-ands with optimized lipophilicity and bind-ing affinity, 593

Recursive partitioning – Classification mod-els for CYP450 3A4 inhibitors andnon–inhibitors, 2354

Reducing power – Synthesis of(±)Abyssinone I and related compounds:Their anti–oxidant and cytotoxic activities,2239

Regioselective – N1–Alkylated 3,4–dihy-dropyrimidine–2(1H)–ones: Convenientone–pot selective synthesis and evaluationof their calcium channel blocking activity,1997 – Natural tanshinone–like hetero-cyclic–fused ortho–quinones from regiose-lective Diels–Alder reaction: Synthesis andcytotoxicity evaluation, 3915

Regression analysis – Antileukotrienicphenethylamido derivatives of arylalkanoicacids in the treatment of ulcerative colitis,332

Renin inhibitors – Application of 3D QSARCoMFA/CoMSIA and in silico dockingstudies on novel renin inhibitors against car-diovascular diseases, 3703

Restrained molecular dynamics – Studies onself–aggregation of anthracycline drugs byrestrained molecular dynamics approachusing nuclear magnetic resonance spec-troscopy supported by absorption, fluores-cence, diffusion ordered spectroscopy andmass spectrometry, 1437

Resveratrol analogs – Synthesis and biologi-cal evaluation of cytotoxic properties of stil-bene–based resveratrol analogs, 701

Resveratrol – A theoretical antioxidant phar-macophore for resveratrol, 1644

Retinoid – Effect of conjugates ofall–trans–retinoic acid and shorter polyenechain analogues with amino acids onprostate cancer cell growth, 3175

Retinoid receptors – Effect of conjugates ofall–trans–retinoic acid and shorter polyenechain analogues with amino acids onprostate cancer cell growth, 3175

Retinoid–related molecules (RRMs) –Highly twisted adamantyl arotinoids:Synthesis, antiproliferative effects and RXRtransactivation profiles, 2434

Retinoids – Preparation of spermine conju-gates with acidic retinoids with potentribonuclease P inhibitory activity, 2689

Retinoyl ferrocene derivatives – Synthesis,characterization and in vitro antiprolifera-tive activities of new 13–cis–retinoyl fer-rocene derivatives, 2572

Reverse transcriptase inhibitor – PredictiveQSAR modeling of HIV reverse transcrip-tase inhibitor TIBO derivatives, 1509

Reverse transcriptase – Thiocarbamates asnon–nucleoside HIV–1 reverse transcrip-tase inhibitors: Docking–based CoMFA andCoMSIA analyses, 2059

RFC – Cytotoxicity and effects of1,10–phenanthroline and5–amino–1,10–phenanthroline derivativeson some immunocompetent cells, 5099

RGD – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394 –Synthesis and biochemical evaluation of acyclic RGD oxorhenium complex as newligand of �V�3 integrin, 3394

RGD octapeptide – Synthesis, evaluation and3D QSAR analysis of novel estradiol–RGDoctapeptide conjugates with oral anti–osteo-porosis activity, 1689

Rhenium – Synthesis and biochemical evalu-ation of a cyclic RGD oxorhenium complexas new ligand of �V�3 integrin, 3394 –Synthesis and characterization of rheniumand technetium–99m tricarbonyl complexesbearing the 4–[3–bromophenyl]quinazolinemoiety as a biomarker for EGFR–TK imag-ing, 4021

Rhodanine – Synthesis and in vivo antidiabet-ic activity of novel dispiropyrrolidinesthrough [3�2] cycloaddition reactions with

Page 46: Chal Micro

5176 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

thiazolidinedione and rhodanine deriva-tives, 3272

Ribonuclease P inhibition – Preparation ofspermine conjugates with acidic retinoidswith potent ribonuclease P inhibitory activi-ty, 2689

Rigid analogues – Tetrahydronaphthyl azoleoxime ethers: The conformationally rigidanalogues of oxiconazole as antibacterials,437

Rimonabant – Analogs of JHU75528, a PETligand for imaging of cerebral cannabinoidreceptors (CB1): Development of ligandswith optimized lipophilicity and bindingaffinity, 593 – The structure of Rimonabantin the solid state and in solution: An experi-mental and theoretical study, 1864

Ring–substituted quinolines – Synthesis,anti–tuberculosis activity and 3D–QSARstudy of amino acid conjugates of4–(adamantan–1–yl) group containingquinolines, 2017

RNA – Simple synthesis of carbon–11 labeledstyryl dyes as new potential PET RNA–spe-cific, living cell imaging probes, 2300

Rosiglitazone – Spectrophotometric andHPLC determinations of anti–diabeticdrugs, rosiglitazone maleate and metforminhydrochloride, in pure form and in pharma-ceutical preparations, 4998

Rota–Rod – Synthesis and antinociceptiveactivities of some pyrazoline derivatives,2606

RP–HPLC – Synthesis and biochemical eval-uation of a cyclic RGD oxorhenium com-plex as new ligand of �V�3 integrin, 3394

Ru(II) complex – Cytotoxic and genotoxiceffects of [Ru(phi)3]2� evaluated byAmes/Salmonella and MTT methods, 2601

Rubiaceae–type cyclopeptides – 2D– and3D–QSAR studies on 54 anti–tumorRubiaceae–type cyclopeptides, 3425

Ruthenium complexes – Effect of rutheniumcomplexation on trypanocidal activity of5–nitrofuryl containing thiosemicar-bazones, 4937

Ruthenium(II) complexes – Synthesis andDNA–binding studies of two ruthenium(II)complexes of an intercalating ligand, 2044

RXR – Highly twisted adamantyl arotinoids:Synthesis, antiproliferative effects and RXRtransactivation profiles, 2434

B�� Receptor ligands – 1,4–Diazepanes derived

from (S)–serine – Homopiperazines withimproved ��1 (sigma) receptor affinity andselectivity, 519 – Synthesis of � receptorligands with unsymmetrical spiro connec-tion of the piperidine moiety, 4306

SSAERs – CoMFA, LeapFrog and blind dock-

ing studies on sulfonanilide derivatives act-ing as selective aromatase expression regu-lators, 3445

Salicylaldehyde – Synthesis, characterization,antimicrobial and antitumor screening ofsome diorganotin(IV) complexes of2–[(9H–Purin–6–ylimino)]–phenol, 3981 –

Synthesis, spectroscopic characterizationand antibacterial activity of new cobalt(II)complexes of unsymmetrical tetradentate(OSN2) Schiff base ligands, 4490

Salicylamide isosteres – QSAR analysis ofsalicylamide isosteres with the use of quan-tum chemical molecular descriptors, 869

SAR – Design, synthesis and structure–activi-ty relationships of antiproliferative 1,3–dis-ubstituted urea derivatives, 453 – Synthesis,biological evaluation and SAR of sulfon-amide 4–methoxychalcone derivatives withpotential antileishmanial activity, 755 –Synthesis and in vitro anti–HIV evaluationof a new series of 6–arylmethyl–substitutedS–DABOs as potential non–nucleosideHIV–1 reverse transcriptase inhibitors,1016 – Novel amide derivatives asinhibitors of histone deacetylase: Design,synthesis and SAR, 1067 – Naturalpolyprenylated benzophenones inhibitingcysteine and serine proteases, 1230 –Examination of growth inhibitory propertiesof synthetic chalcones for which antibacter-ial activity was predicted, 2211 – Synthesisand evaluation of a novel series of hetero-cyclic oleanolic acid derivatives withanti–osteoclast formation activity, 2796

Sarin – In–vitro regeneration of sarin inhibit-ed electric eel acetylcholinesterase bybis–pyridinium oximes bearing xylene link-er, 1326

SARs – Synthesis and in vitro cytotoxic eval-uation of novel 3,4,5–trimethoxyphenylsubstituted �–carboline derivatives, 533

Scanning electron microscopy – Synthesisand activity of fibrillogenesis peptideinhibitors related to the 17–21 �–amyloidsequence, 179

Scavenging/antioxidant activity –Melatonin: Quantum–chemical and bio-chemical investigation of antioxidant activ-ity, 2834

Schiff base – Fullerene derivatized s–triazineanalogues as antimicrobial agents, 2178 –Synthesis and anti–microbial screening ofsome Schiff bases of 3–amino–6,8–dibro-mo–2–phenylquinazolin–4(3H)–ones, 2328– Synthesis of some new 1,3,4–thiadia-zol–2–ylmethyl–1,2,4–triazole derivativesand investigation of their antimicrobialactivities, 2896 – Regioselective reaction:Synthesis and pharmacological study ofMannich bases containing ibuprofen moi-ety, 3697 – Novel4–(morpholin–4–yl)–N'–(arylidene)benzo-hydrazides: Synthesis, antimycobacterialactivity and QSAR investigations, 3954 –Synthesis, characterization, antimicrobialand antitumor screening of some diorgan-otin(IV) complexes of2–[(9H–Purin–6–ylimino)]–phenol, 3981 –Preparation and antitubercular activities invitro and in vivo of novel Schiff bases ofisoniazid, 4169 – Synthesis, spectroscopiccharacterization and antibacterial activity ofnew cobalt(II) complexes of unsymmetricaltetradentate (OSN2) Schiff base ligands,4490 – Synthesis ofsubstituted–phenyl–1,2,4–triazol–3–thioneanalogues with modified d–glucopyranosyl

residues and their antiproliferative activi-ties, 4716

Schiff bases – Synthesis, NMR characteriza-tion and in vitro antitumor evaluation ofnew aminophosphonic acid diesters, 3363 –Regioselective reaction: Synthesis, charac-terization and pharmacological studies ofsome new Mannich bases derived from1,2,4–triazoles, 3784 – Chiral gossypolderivatives: Evaluation of their anticanceractivity and molecular modeling, 3961 –Crystal structures, antioxidation and DNAbinding properties of Dy(III) complexeswith Schiff–base ligands derived from8–hydroxyquinoline–2–carboxaldehydeand four aroylhydrazines, 5080

Schiff’s bases – Synthesis and antitumoractivity of some new xanthotoxin deriva-tives, 2967

Sciatic nerve – Evaluation of the local anaes-thetic activity of 3–aminobenzo[d]isothia-zole derivatives using the rat sciatic nervemodel, 473

SD – Synthesis and biochemical evaluation ofa cyclic RGD oxorhenium complex as newligand of �V�3 integrin, 3394

Seco–tanapartholide – Structure–activityrelationship of seco–tanapartholides isolat-ed from Achillea falcata for inhibition ofHaCaT cell growth, 3794

Selective ligand – Bibenzyl– andstilbene–core compounds with non–polarlinker atom substituents as selective ligandsfor estrogen receptor beta, 3412 – Phenethylpyridines with non–polar internal substitu-tents as selective ligands for estrogen recep-tor beta, 3560

Selenosemicarbazone – Synthesis and char-acterization of new Pt(II) and Pd(II) com-plexes with 2–quinolinecarboxaldehydeselenosemicarbazone: Cytotoxic activityevaluation of Cd(II), Zn(II), Ni(II), Pt(II)and Pd(II) complexes with heteroaromaticselenosemicarbazones, 1623

Self assemblage tendency – Perspectives indesigning anti aggregation agents asAlzheimer disease drugs, 3866

Self–assembled monolayers – Contact–activemicrobicidal gold surfaces using immobi-lization of quaternary ammonium thiolderivatives, 4227

Semicarbazides – Synthesis of some novelN4–(naphtha[1,2–d]thiazol–2–yl)semicar-bazides as potential anticonvulsants, 203

Semi–synthetic 4–nerolidylcatechol deriva-tives – New antimalarial and cytotoxic4–nerolidylcatechol derivatives, 2731

Serine–enzyme inhibition – Large ring1,3–bridged 2–azetidinones: Experimentaland theoretical studies, 2071

Serotonin receptor – Quantitativestructure–activity relationship study of sero-tonin (5–HT7) receptor inhibitors usingmodified ant colony algorithm and adaptiveneuro–fuzzy interference system (ANFIS),1463 – Application of desirability–basedmulti(bi)–objective optimization in thedesign of selective arylpiperazine derivatesfor the 5–HT1A serotonin receptor, 5045

SERT – Synthesis and serotonin transporteractivity of sulphur–substituted �–alkyl

Page 47: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5177

phenethylamines as a new class of anti-cancer agents, 4862

Sesquiterpene lactone – Structure–activityrelationship of seco–tanapartholides isolat-ed from Achillea falcata for inhibition ofHaCaT cell growth, 3794

Sesquiterpene lactones – Synthesis and cyto-toxic activity of �–santonin derivatives,3739

Shikonin derivatives – Synthesis and antitu-mor activity of 6– and 2–(1–substituted–thio–4–methylpent–3–enyl)–5,8–dimethoxynaphthalene–1,4–diones, 1410

Shuffling cross–validation – Quantitativestructure–activity relationship study of sero-tonin (5–HT7) receptor inhibitors usingmodified ant colony algorithm and adaptiveneuro–fuzzy interference system (ANFIS),1463

Single crystal – Synthesis and structure analy-sis of cyclodehydration product of piroxi-cam: A metabolite detected in dogs andmonkeys, 3368

Size–intensive descriptors – Molecular prop-erties of psychopharmacological drugsdetermining non–competitive inhibition of5–HT3A receptors, 2667

Skeletal muscle relaxant activity – Synthesisof novel bioactive derivatives of3–(4–chlorophenyl)–2–hydrazino–5,6,7,8–tetrahydrobenzo(b)thieno[2,3–d]pyrimi-dine–4(3H)–ones, 4721

Skimmin – Antiamoebic coumarins from theroot bark of Adina cordifolia and their newthiosemicarbazone derivatives, 2252

Small peptides – Computational study of theelectronic structure characterization of anovelanti–inflammatory tripeptide derivedfrom monocyte locomotion inhibitoryfactor(MLIF)–pentapeptide, 3114

SMILES – QSPR modeling bioconcentrationfactor (BCF) by balance of correlations,2544

Smooth muscle relaxation – A series of 1,2–coupled indane dimers with mast cell sta-bilisation and smooth muscle relaxationproperties, 5018

S– and C–nucleosidoquinazolines – S– andC–nucleosidoquinazoline as new nucleosideanalogs with potential analgesic andanti–inflammatory activity, 4249

S–Allylthio–6–mercaptopurine – Novelderivatives of 6–mercaptopurine: Synthesis,characterization and antiproliferative activi-ties of S–allylthio–mercaptopurines, 541

S–DABOs – Synthesis and in vitro anti–HIVevaluation of a new series of 6–aryl-methyl–substituted S–DABOs as potentialnon–nucleoside HIV–1 reverse transcrip-tase inhibitors, 1016

S–Methylthiosemicarbazone–oxovanadium– Synthesis, characterization and antidiabet-ic properties of N1–2,4–dihydroxybenzyli-dene–N4–2–hydroxybenzylidene–S–methyl–thiosemicarbazidato–oxovanadium(IV),818

B��–Receptors – Substituted benzo[d]oxa-

zol–2(3H)–one derivatives with prefer-ence for the ��1 binding site, 124

Ss–Triazine – Fullerene derivatized s–triazine

analogues as antimicrobial agents, 2178Sodium channel – 2D– and 3D–QSAR of

Tocainide and Mexiletine analogues actingas Nav1.4 channel blockers, 1477

Solid–phase synthesis – The influence of anethylene spacer on the 5–HT1A and 5–HT2Areceptor affinity of arylpiperazine deriva-tives of amides with N–acylated aminoacids and 3–differently substituted pyrroli-dine–2,5–diones, 800

Solution–phase parallel synthesis (SPPS) –Solution–phase parallel synthesis and eval-uation of anticonvulsant activity of N–sub-stituted–3,4–dihydroisoquinoline–2(1H)–carboxamides, 1349

Solvent effect – Molecular structure and sta-bility of perindopril erbumine and perindo-pril l–arginine complexes, 101

SOMFA – Self organizing molecular fieldanalysis on a series of human 5�–reductaseinhibitors: Unsaturated 3–carboxysteroid,4920

Sonogashira coupling – Synthesis of novel3–(aryl)benzothieno[2,3–c]pyran–1–onesfrom Sonogashira products and intramolec-ular cyclization: Antitumoral activity evalu-ation, 1893

Spectral moments – Multi–target spectralmoment: QSAR for antifungal drugs vs. dif-ferent fungi species, 4051 – Scoring func-tion for DNA–drug docking of anticancerand antiparasitic compounds based on spec-tral moments of 2D lattice graphsfor molec-ular dynamics trajectories, 4461

Spectral – Synthesis, characterization, DNAcleavage and in vitro antimicrobial studies ofLa(III), Th(IV) and VO(IV) complexes withSchiff bases of coumarin derivatives, 2904

Spectral studis – Biological activity studieson metal complexes of novel tridentateSchiff base ligand. Spectroscopic and ther-mal characterization, 4801

Spectrophotometry – A novel spectrophoto-metric method for the determination ofaminophylline with boric acid in pharma-ceutical and mixed serum samples, 1452 –Blue CrO5 assay: A novel spectrophotomet-ric method for the evaluation of the antioxi-dant and oxidant capacity of various biolog-ical substances, 4162

Spectroscopic studies – Antimicrobial activemacrocyclic complexes of Cr(III), Mn(III)and Fe(III) with their spectroscopicapproach, 3299

Spectroscopy – Synthesis, spectroscopic char-acterization, X–ray structure and evaluationof binding parameters of newtriorganotin(IV) dithiocarboxylates withDNA, 3986 – Synthesis, crystal structuresand antibacterial activity studies ofaza–derivatives of phytoalexin from cottonplant – gossypol, 4393

Spermine conjugates – Preparation of sper-mine conjugates with acidic retinoids withpotent ribonuclease P inhibitory activity,2689

Sphere–exclusion – Development of QSARmodels for predicting hepatocarcinogenictoxicity of chemicals, 3658

Spiroazetidinones – Synthesis and antimicro-bial activity of new 1–alkyl/cyclo-hexyl–3,3–diaryl–1'–methylspiro[azeti-dine–2,3'–indoline]–2',4–diones, 2265

Spirocyclic piperidines – Synthesis of �receptor ligands with unsymmetrical spiroconnection of the piperidine moiety, 4306

Spiro–piperidone – A facile synthesis andantimycobacterial evaluation of novelspiro–pyrido–pyrrolizines and pyrrolidines,3821

Spirosuccinimides – The influence of an eth-ylene spacer on the 5–HT1A and 5–HT2Areceptor affinity of arylpiperazine deriva-tives of amides with N–acylated aminoacids and 3–differently substituted pyrroli-dine–2,5–diones, 800

SPPS – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

SPR (surface plasmon resonance) –Computational modeling and surface plas-mon resonance analyses in the assessmentof peptide ligands interacting with fibrin�(312–324) epitope, 2128

SQ109 – Pentacyclo–undecane derived cyclictetra–amines: Synthesis and evaluation aspotent anti–tuberculosis agents, 4297

Src – Discovering novelquercetin–3–O–amino acid–esters as a newclass of Src tyrosine kinase inhibitors, 1982– Determination of permeability andlipophilicity of pyrazolo–pyrimidine tyro-sine kinase inhibitors and correlation withbiological data, 3712

Stability – An in vitro characterization study ofnew near infrared dyes for molecular imag-ing, 3496 – Synthesis, antiviral activity, andstability of nucleoside analogs containing tri-cyclic bases, 3845 – Didanosine ester pro-drugs: Synthesis, albumin binding propertiesand pharmacokinetic studies in rats, 3874

Stabilization energies – A theoretical antioxi-dant pharmacophore for resveratrol, 1644

Staphylococcus aureus – Examination ofgrowth inhibitory properties of syntheticchalcones for which antibacterial activitywas predicted, 2211 – A novel and efficientone step synthesis of2–amino–5–cyano–6–hydroxy–4–arylpyrimidines and their anti–bacterial activity,2651 – Contact–active microbicidal goldsurfaces using immobilization of quaternaryammonium thiol derivatives, 4227

Staurosporine – A three–step synthesis fromrebeccamycin of an efficient checkpointkinase 1 inhibitor, 2234

Sterioselectivity – Stereoselective synthesisand antimicrobial activity ofbenzofuran–based (1E)–1–(piperidin–1–yl)–N2–arylamidrazones, 4985

Steroid – Steroidal lactones as inhibitors of17�–hydroxysteroid dehydrogenase type 5:Chemical synthesis, enzyme inhibitoryactivity, and assessment of estrogenic andandrogenic activities, 632 – Identification ofputative steroid–binding sites in humanABCB1 and ABCG2, 3601 – Self organiz-ing molecular field analysis on a series ofhuman 5�–reductase inhibitors:Unsaturated 3–carboxysteroid, 4920

Page 48: Chal Micro

5178 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Steroidomimetics – Novel CYP17 inhibitors:Synthesis, biological evaluation,structure–activity relationships and model-ling of methoxy– and hydroxy–substitutedmethyleneimidazolyl biphenyls, 2765

Steroids – Novel modified steroid derivativesof androstanolone as chemotherapeuticanti–cancer agents, 3936 – Synthesis andanabolic/androgenic evaluation of novel9�–fluorosteroids, 4567

Stilbenes – Synthesis and biological evalua-tion of cytotoxic properties ofstilbene–based resveratrol analogs, 701

Stilbestrol – Bibenzyl– and stilbene–corecompounds with non–polar linker atom sub-stituents as selective ligands for estrogenreceptor beta, 3412 – Phenethyl pyridineswith non–polar internal substitutents asselective ligands for estrogen receptor beta,3560

Stroke – Design and synthesis of calpaininhibitory 6–pyridone 2–carboxamidederivatives, 1331

Stroke volume – Synthesis of 2–(4–substitut-edmethylpiperazin–1–yl)–N–(3,4–dihy-dro–3–oxo–2H–benzo[b][1,4]oxazin–7–yl)acetamides and their positive inotropic eval-uation, 3027

Structural characterization – Synthesis,characterization and antidiabetic propertiesof N1–2,4–dihydroxybenzylidene–N4–2–hydroxybenzylidene–S–methyl–thiosemicarbazidato–oxovanadium(IV), 818

Structure activity – Synthesis, characterisa-tion and in vitro cytotoxicity studies of aseries of chiral platinum(II) complexesbased on the 2–aminomethylpyrrolidine lig-and: X–ray crystal structure of[ P t C l 2 ( R – d i m e p y r r ) ](R–dimepyrr=N–dimethyl–2(R)–aminomethylpyrrolidine), 2807

Structure elucidation – Novel ureas andthioureas of 15–membered azalides withantibacterial activity against key respiratorypathogens, 3459

Structure–activity relationship (SAR) –Application of phosphonyl carbanions tohighly regioselective synthesis of somediazaphospholes and pyrazolinyl phospho-nates, 526 – Synthesis, structure and struc-ture–activity relationship analysis of3–tert–butoxycarbonyl–2–arylthiazoli-dine–4–carboxylic acid derivatives aspotential antibacterial agents, 3903

Structure–activity relationship – The syn-thesis of N–phenoxyethyl–1–substitut-ed–1,2,3,4–tetrahydroisoquinolines andtheir �1–adrenoceptor blocking activity,1271 – Synthesis and antitumor activity of6– and 2–(1–substituted–thio–4–methylpent–3–enyl)–5,8–dimethoxynaph-thalene–1,4–diones, 1410 – Synthesis, char-acterization and structure–activity relation-ship analysis of novel depsides as potentialantibacterials, 1779 – Studies on chemicalstructure modification and biology of a nat-ural product, Gambogic acid (I): Synthesisand biological evaluation of oxidized ana-logues of gambogic acid, 2611 –Structure–based virtual screening approachto identify novel classes of PTP1B

inhibitors, 3280 – Structure–activity rela-tionship of seco–tanapartholides isolatedfrom Achillea falcata for inhibition ofHaCaT cell growth, 3794 – Novel2,4,5–trisubstituted oxazole derivatives:Synthesis and antiproliferative activity,3930 – Antinociceptive properties of caffeicacid derivatives in mice, 4596 – Anti–nitricoxide production activity of isothiocyanatescorrelates with their polar surface arearather than their lipophilicity, 4931 –Amines and oximes derived from deoxy-benzoins as Helicobacter pylori ureaseinhibitors, 2246 – Chiral gossypol deriva-tives: Evaluation of their anticancer activityand molecular modeling, 3961 – Facile syn-thesis and in vitro properties of 1–alkyl–and 1–alkyl–N–propargyl–1,2,3,4–tetrahy-droisoquinoline derivatives on PC12 cells,4034 – Structure–activity relationship ofdopaminergic halogenated1–benzyl–tetrahydroisoquinoline deriva-tives, 4616

Structure–affinity relationships – Synthesisof � receptor ligands with unsymmetricalspiro connection of the piperidine moiety,4306

Structure–cytotoxicity–fluorescence relation-ship – Design, cytotoxic and fluorescentproperties of novel N–phosphorylalkyl substi-tuted E,E–3,5–bis(arylidene)piperid–4–ones,2135

Structure–property–activity relationshipmodel – Molecular properties of psy-chopharmacological drugs determiningnon–competitive inhibition of 5–HT3Areceptors, 2667

Strychnine – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Design, synthesis of 8–alkoxy–5,6–dihy-dro–[1,2,4]triazino[4,3–a]quinolin–1–oneswith anticonvulsant activity, 1265

Styryl benzimidazole – Synthesis and evalu-ation of in vitro anti–microbial andanti–tubercular activity of 2–styryl benzim-idazoles, 4244

Styryl dyes – Simple synthesis of carbon–11labeled styryl dyes as new potential PETRNA–specific, living cell imaging probes,2300

Styryl – Synthesis of some new 4–styryltetra-zolo[1,5–a]quinoxaline and 1–substitut-ed–4–styryl[1,2,4]triazolo[4,3–a]quinoxa-line derivatives as potent anticonvulsants,1135

STZ–S model – Synthesis of �–amyrin deriv-atives and their in vivo antihyperglycemicactivity, 1215

Subcutaneous pentylenetetrazole inducedseizure – Synthesis, anticonvulsant andCNS depressant activity of some new bioac-tive 1–(4–substituted–phenyl)–3–(4–oxo–2–pheny l /e thy l–4H–quina-zolin–3–yl)–urea, 4335

Subcutaneous pentylenetetrazole–inducedseizure – Synthesis and anticonvulsantactivity of some substituted 1,2,4–thiadia-zoles, 1100

Substituted benzimidazoles – Synthesis andQSAR evaluation of 2–(substituted

phenyl)–1H–benzimidazoles and [2–(sub-stituted phenyl)–benzimidazol–1–yl]–pyridin–3–yl–methanones, 1119

Substituted hydrazides – Hansch analysis ofsubstituted benzoic acidbenzyl idene / furan–2–yl–methylenehydrazides as antimicrobial agents, 1853

Substituted imidazoles – Synthesis, antimi-crobial and antiviral evaluation of substitut-ed imidazole derivatives, 2347

Substituted oxy/thio acetic acid ethyl esters– Synthesis of some novel bioactive4 – o x y / t h i osubstituted–1H–pyrazol–5(4H)–ones viaefficient cross–Claisen condensation, 3852

Substrate inhibition – The metabolism ofCYP2C9 and CYP2C19 for gliclazide byhomology modeling and docking study, 854

Substrate properties – Evaluation of sub-strate and inhibitor properties of a novelMDR modulator H17 towards transmem-brane efflux pumps, 3060

Succinimide – Synthesis and antimicrobialactivity of some new N–acyl substitutedphenothiazines, 5094

Succinimides – The influence of an ethylenespacer on the 5–HT1A and 5–HT2A receptoraffinity of arylpiperazine derivatives ofamides with N–acylated amino acids and3–differently substitutedpyrrolidine–2,5–diones, 800

Sulfamide – Synthesis and pharmacologicalevaluation of sulfamide–based analogues ofanandamide, 4889

Sulfonamide 4–methoxychalcones –Synthesis, biological evaluation and SAR ofsulfonamide 4–methoxychalcone deriva-tives with potential antileishmanial activity,755

Sulfonamide – Synthesis and biological eval-uation of a new family of anti–benzylanili-nosulfonamides as CA IX inhibitors, 511 –Design, synthesis and anticancer evaluationof novel tetrahydroquinoline derivativescontaining sulfonamide moiety, 4211

Sulfonamides – A QSAR study on relation-ship between structure of sulfonamides andtheir carbonic anhydrase inhibitory activityusing the eigenvalue (EVA) method, 3439

Sulfonanilide – CoMFA, LeapFrog and blinddocking studies on sulfonanilide derivativesacting as selective aromatase expressionregulators, 3445

Sulfonyl chlorides – Synthesis and in vitroantiproliferative activity of novel 1–ben-zhydrylpiperazine derivatives againsthuman cancer cell lines, 1223

Sulfonylurea – Synthesis and blood glucoselowering effect of novel pyridazinone sub-stituted benzenesulfonylurea derivatives,2673

Sulfur/selenium–benzo[h]quinolines –Synthesis of novel benzo[h]quinolines:Wound healing, antibacterial, DNA bindingand in vitro antioxidant activity, 981

Sulindac analogues – Synthesis, pharmaco-logical evaluation and docking studies ofnew sulindac analogues, 1959

Sulphur atoms – Known drug space as a met-ric in exploring the boundaries of drug–likechemical space, 5006

Page 49: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5179

Superoxide anion generation – Oligomericformylpeptide activity on human neu-trophils, 4926

Superoxide dismutase activity –Antimicrobial and SOD activities of noveltransition metal ternary complexes of imin-odiacetic acid containing �–diimine as aux-iliary ligand, 2517

Superoxide dismutase – Copper complexesof pyridine derivatives with superoxidescavenging and antimicrobial activities,3259

Support vector classification (SVC) – QSARstudy of Akt/protein kinase B (PKB)inhibitors using support vector machine,4090

Support vector machine (SVM) – QSARstudy of Akt/protein kinase B (PKB)inhibitors using support vector machine,4090

Support vector machine – Application ofgenetic algorithm–support vector machine(GA–SVM) for prediction of BK–channelsactivity, 5023

Support vector regression (SVR) – QSARstudy of Akt/protein kinase B (PKB)inhibitors using support vector machine,4090

Supramolecular framework – Antimicrobialand SOD activities of novel transition metalternary complexes of iminodiacetic acidcontaining �–diimine as auxiliary ligand,2517

Surfactant – An investigation into the role ofsurfactants in controlling particle size ofpolymeric nanocapsules containing peni-cillin–G in double emulsion, 2392

Surfactants – Preparation and antimicrobialbehaviour of quaternary ammonium thiolderivatives able to be grafted on metal sur-faces, 717 – Cationic surfactants fromlysine: Synthesis, micellization and biologi-cal evaluation, 1884 – Synthesis and antimi-crobial properties of polymerizable quater-nary ammoniums, 3201

Surfmers – Synthesis and antimicrobial prop-erties of polymerizable quaternary ammoni-ums, 3201

Sustained drug delivery – PEGylated PPIdendritic architectures for sustained deliv-ery of H2 receptor antagonist, 1155

SVM – Prediction of CCR5 receptor bindingaffinity of substituted 1–(3,3–diphenyl-propyl)–piperidinyl amides and ureas basedon the heuristic method, support vectormachine and projection pursuit regression,25 – QSAR models for 2–amino–6–arylsul-fonylbenzonitriles and congeners HIV–1reverse transcriptase inhibitors based on lin-ear and nonlinear regression methods, 2158

Symmetrical bis–benzimidazole – Design,synthesis, and anti–tumor evaluation ofnovel symmetrical bis–benzimidazoles,1808

Synthesis – Design, synthesis and AChEinhibitory activity of indanone and auronederivatives, 7 – Synthesis and anti–HIV–1integrase activities of 3–aroyl–2,3–dihy-dro–1,1–dioxo–1,4,2–benzodithiazines, 190– Synthesis of new series of5,6–dihydro–4H–1,2–oxazines via hetero

Diels–Alder reaction and evaluation ofantimicrobial activity, 280 – Synthesis,cytotoxicity and apoptosis of naphthalimidepolyamine conjugates as antitumor agents,393 – Synthesis and in vitro cytotoxic eval-uation of novel 3,4,5–trimethoxyphenylsubstituted �–carboline derivatives, 533 –Discovery of a new family ofbis–8–hydroxyquinoline substituted benzy-lamines with pro–apoptotic activity in can-cer cells: Synthesis, structure–activity rela-tionship, and action mechanism studies, 558– Design, synthesis and evaluation of galan-thamine derivatives as acetylcholinesteraseinhibitors, 772 – Synthesis and adrenolyticactivity of1–(1H–indol–4–yloxy)–3–{[2–(2–methoxyphenoxy)ethyl]amino}propan–2–ol and itsenantiomers. Part 1, 809 – Synthesis andbiological evaluation of novel luteolinderivatives as antibacterial agents, 908 –Synthesis and QSAR evaluation of 2–(sub-stituted phenyl)–1H–benzimidazoles and[ 2 – ( s u b s t i t u t e dphenyl)–benzimidazol–1–yl]–pyridin–3–yl–methanones, 1119 – Synthesis and antitu-mor activity of 6– and2–(1–substituted–thio–4–methylpent–3–enyl)–5,8–dimethoxynaphthalene–1,4–diones,1410 – Synthesis of chlorovinyl sulfones asstructural analogs of chalcones and theirantiplasmodial activities, 1457 – Synthesisand antibacterial evaluation of novel4–alkyl substituted phenyl �–aldehydeketone derivatives, 1737 – A class of potenttyrosinase inhibitors:Alkylidenethiosemicarbazide compounds,1773 – Design, synthesis, and evaluation ofbiphenyl–4–yl–acrylohydroxamic acidderivatives as histone deacetylase (HDAC)inhibitors, 1900 – Design, synthesis, andbiological evaluation of novel triazolederivatives as inhibitors of cytochromeP450 14�–demethylase, 1913 – Newinsights into the antioxidant activity ofhydroxycinnamic acids: Synthesis andphysicochemical characterization of novelhalogenated derivatives, 2092 – Design,cytotoxic and fluorescent properties ofnovel N–phosphorylalkyl substitutedE,E–3,5–bis(arylidene)piperid–4–ones,2135 – Design, synthesis and antibacterialactivity of novel actinonin derivatives con-taining benzimidazole heterocycles, 2202 –Synthesis and biological activity evaluationof 1H–benzimidazoles via mammalianDNA topoisomerase I and cytostaticityassays, 2280 – Synthesis, characterizationand antitumor activity of new type binuclearplatinum(II) complexes, 2322 – Substitutedquinazolines, part 3. Synthesis, in vitro anti-tumor activity and molecular modelingstudy of certain 2–thieno–4(3H)–quinazoli-none analogs, 2379 – Highly twistedadamantyl arotinoids: Synthesis, antiprolif-erative effects and RXR transactivation pro-files, 2434 – Synthesis, biological evalua-tion and molecular modeling of oxoisoapor-phine and oxoaporphine derivatives as newdual inhibitors ofacetylcholinesterase/butyrylcholinesterase,

2523 – Synthesis, characterization and invitro antiproliferative activities of new13–cis–retinoyl ferrocene derivatives, 2572– Synthesis, characterization and cytotoxic-ity of ammine/ethylamine platinum(II)complexes with carboxylates, 2758 –Synthesis, antifungal activities and3D–QSAR study of N–(5–substitut-ed–1,3,4–thiadiazol–2–yl)cyclopropanecar-boxamides, 2782 – Synthesis and biologicalevaluation of a novel series of 1,5–benzoth-iazepine derivatives as potential antimicro-bial agents, 2815 – Synthesis, characteriza-tion, DNA cleavage and in vitro antimicro-bial studies of La(III), Th(IV) and VO(IV)complexes with Schiff bases of coumarinderivatives, 2904 – Investigation of theantioxidant properties of some new4–hydroxycoumarin derivatives, 3077 –Recent developments in the design and syn-thesis of hybrid molecules basedon amino-quinoline ring and their antiplasmodialevaluation, 3091 – Synthesis andanti–HSV–1 evaluation of some pyrazolesand fused pyrazolopyrimidines, 3285 –Synthesis and anti–VZV activity of 6–het-eroaryl derivatives of tricyclic acyclovir and9–{[cis–1',2'–bis(hydroxymethyl)cyclo-prop–1'–yl]methyl}guanine analogues,3313 – Mono and bis–6–arylbenzimida-zo[1,2–c]quinazolines: A new class ofantimicrobial agents, 3330 – Aziridine alka-loids as potential therapeutic agents, 3373 –Synthesis, spectral characterization,in–vitro microbiological evaluation andcytotoxic activities of novel macrocyclic bishydrazone, 3552 – Synthesis and antiviralactivity of new pyrazole and thiazole deriv-atives, 3746 – Synthesis and bioactivity ofsubstituted indan–1–ylideneaminoguani-dine derivatives, 3771 – Didanosine esterprodrugs: Synthesis, albumin binding prop-erties and pharmacokinetic studies in rats,3874 – Novel 2,4,5–trisubstituted oxazolederivatives: Synthesis and antiproliferativeactivity, 3930 – Synthesis and antibacterialactivity of novel 15–membered macrolidederivatives: 4"–Carbamate, 11,12–cycliccarbonate–4"–carbamate and11,4"–di–O–arylcarbamoyl analogs ofazithromycin, 4010 – Synthesis and in vitroantibacterial activity of 7–(4–alkoxyimi-no–3–amino–3–methylpiperidin–1–yl)fluo-roquinolone derivatives, 4063 – A new classof anticonvulsants possessing 6Hz activity:3,4–Dialkyloxy thiophene bishydrazones,4376 – Synthesis and antibacterial activityof some new thiadiaza/triazaphospholes,thiadiaza/triaza/tetrazaphosphinines andthiadiaza/tetrazaphosphepines containing1,2,4–triazinone moiety, 4539 – Design,synthesis and in vitro antibacterial/antifun-gal evaluation of novel1–ethyl–6–fluo-ro–1,4–dihydro–4–oxo–7(1–piperazinyl)quinoline–3–carboxylicacid derivatives, 4726– Synthesis, cytotoxicity and DNA–bindinglevels of new type binuclear platinum(II)complexes, 4772 – Synthesis and anticanceractivity ofN–bis(trifluoromethyl)alkyl–N'–thiazolyland N–bis(trifluoromethyl)alkyl–N'–ben-

Page 50: Chal Micro

5180 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

zothiazolyl ureas, 4944 – Synthesis andadrenolytic activity of1–(1H–indol–4–yloxy)–3–(2–(2–methoxyphenoxy)ethylamino)propan–2–ol analogsand its enantiomers. Part 2, 5103

TTarget specific – 10H–Phenothiazines: A new

class of enzyme inhibitors for inflammatorydiseases, 197

Tautomerism – Synthesis, crystal structuresand antibacterial activity studies ofaza–derivatives of phytoalexin from cottonplant – gossypol, 4393

Taxoids – A QSAR study for the cytotoxicactivities of taxoids against macrophage(M)–like cells, 274

Taxol – In vitro and in vivo anticancer activityof 2–deacetoxytaxinine J and synthesis ofnovel taxoids and their in vitro anticanceractivity, 3947

Taxus wallichiana – In vitro and in vivo anti-cancer activity of 2–deacetoxytaxinine Jand synthesis of novel taxoids and their invitro anticancer activity, 3947

TEA – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

Technetium – Synthesis and biochemicalevaluation of a cyclic RGD oxorheniumcomplex as new ligand of �V�3 integrin,3394 – Synthesis and characterization ofrhenium and technetium–99m tricarbonylcomplexes bearing the 4–[3–bro-mophenyl]quinazoline moiety as a biomark-er for EGFR–TK imaging, 4021

Telomerase – Prediction of telomeraseinhibitory activity for acridinic derivativesbased on chemical structure, 4826

Telomere – Synthesis and biological evalua-tion of novel4,5–bis(dialkylaminoalkyl)–substitutedacridines as potent telomeric G–quadruplexligands, 3880

Terephthalic dihydrazide – Synthesis andantibacterial activity of some novelbis–1,2,4–triazolo[3,4–b]–1,3,4–thiadia-zoles and bis–4–thiazolidinone derivativesfrom terephthalic dihydrazide, 5112

Ternary complex – Mechanistic aspects ofbenzothiazepines: A class of antiarrhythmicdrugs, 1

Terpenoid diol – Cytotoxic, antioxidant activ-ities and structure activity relationship ofsome newly synthesized terpenoidal oxali-platin analogs, 901

Testosterone – Steroidal lactones as inhibitorsof 17�–hydroxysteroid dehydrogenase type5: Chemical synthesis, enzyme inhibitoryactivity, and assessment of estrogenic andandrogenic activities, 632 – Self organizingmolecular field analysis on a series ofhuman 5�–reductase inhibitors:Unsaturated 3–carboxysteroid, 4920

Tetrabutylammonium hydrogen sulfate –N 1 – A l k y l a t e d3,4–dihydropyrimidine–2(1H)–ones:Convenient one–pot selective synthesis andevaluation of their calcium channel block-ing activity, 1997

Tetracyclic pyrimidines – Synthesis, anal-gesic and anti–inflammatory activities eval-uation of some bi–, tri– and tetracyclic con-densed pyrimidines, 4572

Tetrahydrobenzimidazoles – Convenientone–pot synthesis of novel 2–substitutedbenzimidazoles, tetrahydrobenzimidazolesand imidazoles and evaluation of their invitro antibacterial and antifungal activities,1751

Tetrahydrobenzofurobenzopyrone –Tetrahydrobenzo– and benzofurobenzopy-rones as a new class of potential photore-agents toward DNA, 18

Tetrahydroisoquinoline – A class of novelN–(3S–1,2,3,4–tetrahydroisoquinoline–3–carbonyl)–l–amino acid derivatives: theirsynthesis, anti–thrombotic activity evalua-tion, and 3D QSAR analysis, 4904

Tetrahydro–4H–chromenes – A facileone–pot green synthesis and antibacterialactivity of 2–amino–4H–pyrans and2–amino–5–oxo–5,6,7,8–tetrahydro–4H–chromenes, 3805

Tetrahydronaphthyl oxime ethers –Tetrahydronaphthyl azole oxime ethers: Theconformationally rigid analogues of oxi-conazole as antibacterials, 437

Tetrahydro–��–carbolines – Comparativestudy of the trypanocidal activity of them e t h y l1–nitrophenyl–1,2,3,4–9H–tetrahydro–��–carboline–3–carboxylate derivatives andbenznidazole using theoretical calculationsand cyclic voltammetry, 1745

Tetrahydropyrans – Design, synthesis andevaluation of tetrahydropyran basedCOX–1/–2 inhibitors, 1278

Tetrazolo – Synthesis of some new 4–styrylte-trazolo[1,5–a]quinoxaline and 1–substitut-ed–4–styryl[1,2,4]triazolo[4,3–a]quinoxa-line derivatives as potent anticonvulsants,1135

TFA – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

Thalidomide – Discovering a new analogueof thalidomide which may be used as apotent modulator of TNF–� production,3533

Theophylline – Synthesis and preliminarypharmacological evaluation of imida-zo[2,1–f]purine–2,4–dione derivatives,4288

Theoretical calculations – Comparativestudy of the trypanocidal activity of themethyl 1–nitrophenyl–1,2,3,4–9H–tetrahy-dro–�–carboline–3–carboxylate derivativesand benznidazole using theoretical calcula-tions and cyclic voltammetry, 1745

Therapy – In vitro and in vivo antitrypanoso-matid activity of 5–nitroindazoles, 1034

Thermal analyses – Biological activity stud-ies on metal complexes of novel tridentateSchiff base ligand. Spectroscopic and ther-mal characterization, 4801

Thermodynamic parameters – Studies onthe interaction of caffeine with bovinehemoglobin, 2100

Thiadiazole – Synthesis and molluscicidalactivity of some new thiophene, thiadiazole

and pyrazole derivatives, 1250 – Synthesisand evaluation of some new benzimidazolederivatives as potential antimicrobialagents, 2294

Thiadiazole thioacetanilides – Synthesis andanti–HIV activity evaluation of 2–(4–(naph-thalen–2–yl)–1,2,3–thiadiazol–5–ylthio)–N–acetamides as novel non–nucleosideHIV–1 reverse transcriptase inhibitors,4648

Thiadiazoles – Synthesis, antiarrhythmic andanticoagulant activities of novel thiazoloderivatives from methyl2–(thiazol–2–ylcarbamoyl)acetate, 725

Thiazine – l–Proline–catalysed facile greenprotocol for the synthesis and antimycobac-terial evaluation of [1,4]–thiazines, 4978

Thiazole derivatives – Adamantane deriva-tives of thiazolyl–N–substituted amide, aspossible non–steroidal anti–inflammatoryagents, 1198

Thiazole – Design, synthesis and characteriza-tion of novel 2–(2,4–disubstituted–thia-zole–5–yl)–3–aryl–3H–quinazoline–4–onederivatives as inhibitors of NF–�B andAP–1 mediated transcription activation andas potential anti–inflammatory agents, 2184– Synthesis and antiviral activity of newpyrazole and thiazole derivatives, 3746 –Synthesis, spectral and biological evalua-tion of some new thiazolidinones and thia-zoles based ont–3–alkyl–r–2,c–6–diarylpiperidin–4–ones,4199 – Synthesis and antibacterial activityof some new thiazole and thiophene deriva-tives, 4434

Thiazoles – Synthesis, antiarrhythmic andanticoagulant activities of novel thiazoloderivatives from methyl2–(thiazol–2–ylcarbamoyl)acetate, 725

Thiazolidine – Synthesis, structure and struc-ture–activity relationship analysis of3–tert–butoxycarbonyl–2–arylthiazoli-dine–4–carboxylic acid derivatives aspotential antibacterial agents, 3903

Thiazolidinedione – Synthesis and in vivoantidiabetic activity of novel dispiropyrro-lidines through [3�2] cycloaddition reac-tions with thiazolidinedione and rhodaninederivatives, 3272

Thiazolidin–4–ones – Synthesis andanti–HIV studies of 2– and3 – a d a m a n t y l – s u b s t i t u t e dthiazolidin–4–ones, 303

Thiazolidinone – Predicting anti–HIV activi-ty of 1,3,4–thiazolidinone derivatives:3D–QSAR approach, 1180 – Synthesis andbiological evaluation of some thiazolidi-none derivatives of steroid as antibacterialagents, 2597 – Synthesis, spectral and bio-logical evaluation of some new thiazolidi-nones and thiazoles based ont–3–alkyl–r–2,c–6–diarylpiperidin–4–ones,4199 – Synthesis and antibacterial activityof some new thiazole and thiophene deriva-tives, 4434

Thiazolidinones – Synthesis and anti–inflam-matory activity of newer quinazolin–4–onederivatives, 83 – Synthesis and antitumoractivity of some new xanthotoxin deriva-tives, 2967 – Synthesis and pharmacologi-

Page 51: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5181

cal evaluation of novel N–alkyl/aryl substi-tuted thiazolidinone arecoline analogues asmuscarinic receptor 1 agonist inAlzheimer’s dementia models, 4848

Thiazoline – Synthesis and antibacterial activ-ity of some new thiazole and thiophenederivatives, 4434

Thiazolo[3',2':1,2]– and 2,3–dihydroisoxa-zolo[4",5":5',4']thiazolo[3',2':1,2]pyrimi-do[4,5–b]quinolones – Design and synthe-sis of azolopyrimidoquinolines, pyrimido-quinazolines as anti–oxidant, anti–inflam-matory and analgesic activities, 609

Thiazolones – Synthesis of novel thia-zolone–based compounds containing pyra-zoline moiety and evaluation of their anti-cancer activity, 1396

Thiazolopyrimidine – Synthesis of some ureaand thiourea derivatives of3–phenyl/ethyl–2–thioxo–2,3–dihydrothia-zolo[4,5–d]pyrimidine and their antagonis-tic effects on haloperidol–induced catalepsyand oxidative stress in mice, 3889

Thiazolotriazole – Synthesis, analgesic,anti–inflammatory and antimicrobial stud-ies of 2,4–dichloro–5–fluorophenyl con-taining thiazolotriazoles, 827 – Synthesis,characterization and evaluation of antibac-terial activity of somethiazolo[3,2–b][1,2,4]triazole incorporatingdiphenylsulfone moieties, 4752

Thiazolyl–pyrazoline – Synthesis and antimi-crobial evaluation of1–(benzofuran–2–yl)–4–nitro–3–arylbu-tan–1–ones and3–(benzofuran–2–yl)–4,5–dihydro–5–aryl–1–[4–(aryl)–1,3–thiazol–2–yl]–1H–pyra-zoles, 2632

Thieno[3,2–e]pyrimidine – Synthesis ofnovel bioactive derivatives of3–(4–chlorophenyl)–2–hydrazino–5,6,7,8–tetrahydrobenzo(b)thieno[2,3–d]pyrimi-dine–4(3H)–ones, 4721

Thiobarbiturate – Inhibitory effects of5–benzylidene barbiturate derivatives onmushroom tyrosinase and their antibacterialactivities, 4235

Thiocarbamates – Thiocarbamates asnon–nucleoside HIV–1 reverse transcrip-tase inhibitors: Docking–based CoMFA andCoMSIA analyses, 2059

Thiocarbamoyl – Synthesis, spectral studiesand antiamoebic activity of new 1–N–sub-stituted thiocarbamoyl–3–phenyl–2–pyra-zolines, 417 – Bis–pyrazolines: Synthesis,characterization and antiamoebic activity asinhibitors of growth of Entamoeba histolyt-ica, 426 – Synthesis and molluscicidalactivity of some new thiophene, thiadiazoleand pyrazole derivatives, 1250

Thiols – Preparation and antimicrobial behav-iour of quaternary ammonium thiol deriva-tives able to be grafted on metal surfaces,717

Thiophene bishydrazones – A new class ofanticonvulsants possessing 6Hz activity:3,4–Dialkyloxy thiophene bishydrazones,4376

Thiophene – Synthesis and molluscicidalactivity of some new thiophene, thiadiazoleand pyrazole derivatives, 1250 – Synthesis

and anticonvulsant activity of some newbishydrazones derived from 3,4–dipropy-loxythiophene, 3672 – Synthesis and anti-bacterial activity of some new thiazole andthiophene derivatives, 4434

Thiosemicarbazide – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Design, synthesis of 8–alkoxy–5,6–dihy-dro–[1,2,4]triazino[4,3–a]quinolin–1–oneswith anticonvulsant activity, 1265

Thiosemicarbazonato complexes – In vitroand in vivo antitumor activity ofplatinum(II) complexes with thiosemicar-bazones derived from 2–formyl and2–acetyl pyridine and containing ring incor-porated at N(4)–position: Synthesis, spec-troscopic study and crystal structure of plat-inum(II) complexes with thiosemicar-bazones, potential anticancer agents, 1296

Thiosemicarbazone – Synthesis, spectralstudies and in vitro antibacterial activity ofsteroidal thiosemicarbazone and their palla-dium (Pd (II)) complexes, 2270 – Synthesisand biological evaluation of some thiazo-lidinone derivatives of steroid as antibacter-ial agents, 2597

Thiosemicarbazones – Gallium(III) complex-es of 2–pyridineformamide thiosemicar-bazones: Cytotoxic activity against malig-nant glioblastoma, 1870 – Antiamoebiccoumarins from the root bark of Adinacordifolia and their new thiosemicarbazonederivatives, 2252

Thiourea – Synthesis and antitumor activityof optically active thiourea and their2–aminobenzothiazole derivatives: A novelclass of anticancer agents, 2923 – Synthesis,antiviral and anticancer activity of somenovel thioureas derivedfromN–(4–nitro–2–phenoxyphenyl)–methane-sulfonamide, 3591 – Synthesis of some ureaand thiourea derivatives of3–phenyl/ethyl–2–thioxo–2,3–dihydrothia-zolo[4,5–d]pyrimidine and their antagonis-tic effects on haloperidol–induced catalepsyand oxidative stress in mice, 3889 – Searchfor new pharmacophores for antimalarialactivity. Part III: Synthesis and bioevalua-tion of new 6–thioureido–4–anilinoquinazo-lines, 4404 – Antitumor and antimycobacte-rial activities of cyclopalladated complexes:X–ray structure of[ P d ( C 2 , N – d m b a ) ( B r ) ( t u ) ](dmba=N ,N–d ime thy lbenzy lamine ,tu=thiourea), 4611

Thioureas – Novel ureas and thioureas of15–membered azalides with antibacterialactivity against key respiratory pathogens,3459

Thioxopyridine – New pyridone, thioxopyri-dine, pyrazolopyridine and pyridine deriva-tives that modulate inflammatory mediatorsin stimulated RAW 264.7 murinemacrophage, 4547

TIBO derivatives – Predictive QSAR model-ing of HIV reverse transcriptase inhibitorTIBO derivatives, 1509

TIPS – Synthesis and biochemical evaluationof a cyclic RGD oxorhenium complex asnew ligand of �V�3 integrin, 3394

TNBS–induced colitis – Colon–specificmutual amide prodrugs of 4–aminosalicylicacid for their mitigating effect on experi-mental colitis in rats, 131

T–cell epitopes – A set of new amino aciddescriptors applied in prediction of MHCclass I binding peptides, 1144

TNF–�� – Rare dipeptide and urea deriva-tives from roots of Moringa oleifera aspotential anti–inflammatory andantinociceptive agents, 432 – Discoveringa new analogue of thalidomide whichmay be used as a potent modulator ofTNF–�� production, 3533

Tocainide – 2D– and 3D–QSAR of Tocainideand Mexiletine analogues acting as Nav1.4channel blockers, 1477

TOP1–targeting agents – Novel topoiso-merase I–targeting antitumor agents synthe-sized from the N,N,N–trimethylammoniumderivative of ARC–111,5H–2,3–dimethoxy–8,9–methylene-dioxy–5–[(2–N,N,N–trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin–6–oneiodide, 3433

Topoisomerase II – DNA–targeting pyrrolo-quinoline–linked butenone and chalcones:Synthesis and biological evaluation, 2854

Topoisomerase I–targeting agents –Cytotoxicity and TOP1–targeting activity of8– and 9–amino derivatives of 5–butyl– and5–(2–N,N–dimethylamino)ethyl–5H–diben-zo[c,h][1,6]naphthyridin–6–ones, 1471

Total synthesis – Total synthesis and anti-cancer activity of highly potent novel gly-colipid derivatives, 3120

Toxic and promiscuous chemical moieties –Investigation of the incidence of “undesir-able” molecular moieties for high–through-put screening compound libraries in market-ed drug compounds, 1128

Toxicity – Synthesis, spectral characterization,in–vitro microbiological evaluation andcytotoxic activities of novel macrocyclic bishydrazone, 3552 – Synthesis and anticon-vulsant activity of some new bishydrazonesderived from 3,4–dipropyloxythiophene,3672

Transcriptional activation – 3D–QSARstudies on the inhibitors of AP–1 andNF–�B mediated transcriptional activation,2888

Transforming growth factor–�� (TGF–�) –Synthesis and biological evaluation ofb e n z e n e s u l f o n a m i d e – s u b s t i t u t e d4–(6–alkylpyridin–2–yl)–5–(quinox-alin–6–yl)imidazoles as transforminggrowth factor–�� type 1 receptor kinaseinhibitors, 568

Transforming growth factor–�� type I recep-tor – Pharmacophore modeling and virtu-al screening for the discovery of newtransforming growth factor–�� type Ireceptor (ALK5) inhibitors, 4259

Transition metal complexes – New transitionmetal ion complexes with benzimida-zole–5–carboxylic acid hydrazides withantitumor activity, 1500 – Biological activi-ty studies on metal complexes of novel tri-dentate Schiff base ligand. Spectroscopicand thermal characterization, 4801

Page 52: Chal Micro

5182 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Transmetallation – Synthesis of � receptorligands with unsymmetrical spiro connec-tion of the piperidine moiety, 4306

Transmission electron microscopy – Phasetransfer catalyzed synthesis of bis–quino-lines: Antileishmanial activity in experi-mental visceral leishmaniasis and in vitroantibacterial evaluation, 845

trans–Stilbene derivatives – Synthesis ofnovel trans–stilbene derivatives and evalua-tion of their potent antioxidant and neuro-protective effects, 3166

Transport proteins – Synthesis of a series ofN6–substituted adenosines with activityagainst trypanosomatid parasites, 3665

Treatment of ulcerative colitis –Antileukotrienic phenethylamido deriva-tives of arylalkanoic acids in the treatmentof ulcerative colitis, 332

Triazene – Towards an efficient prodrug of thealkylating metabolite monomethyltriazene:Synthesis and stability of N–acylamino acidderivatives of triazenes, 1049

Triazenes – Dopamine– and tyramine–basedderivatives of triazenes: Activation bytyrosinase and implications for prodrugdesign, 3228

Triazepine – Synthesis and antibacterialactivity of some new heterocycles incorpo-rating phthalazine, 4448

Triazine – Synthesis and antibacterial activityof some new heterocycles incorporatingphthalazine, 4448

Triazole – Design and synthesis of5–alkoxy–[1,2,4]triazolo[4,3–a]quinolinederivatives with anticonvulsant activity, 954– Design, synthesis, and biological evalua-tion of novel triazole derivatives asinhibitors of cytochrome P45014�–demethylase, 1913 – Design, synthe-sis, and antifungal activity of triazole andbenzotriazole derivatives, 3064

Triazolopyrimidines derivatives –Analgesic, anticonvulsant and anti–inflam-matory activities of some synthesized ben-zodiazipine, triazolopyrimidine andbis–imide derivatives, 4787

Triazolopyrimidines – Organoiodine(III)–mediated synthesis of 3–aryl/het-eroaryl–5,7–dimethyl–1,2,4–triazolo[4,3–c]pyrimidines as antibacterial agents, 2260

Triazolothiadiazines – Synthesis of 3,6–dis-ubstituted 7H–1,2,4–triazolo[3,4–b]–1,3,4–thiadiazines as novel anal-gesic/anti–inflammatory compounds, 4528

Triazolothiadiazole – Synthesis and antimi-crobial activities of some new triazolothia-diazoles bearing 4–methylthiobenzyl moi-ety, 551

Triazone – Design, synthesis of8–alkoxy–5,6–dihydro–[1,2,4]triazino[4,3–a]quinolin–1–ones with anticonvulsantactivity, 1265

Trichomonas vaginalis – Synthesis and invitro trichomonicidal, giardicidal and ame-bicidal activity of N–acetamide(sulfon-amide)–2–methyl–4–nitro–1H–imidazoles,2975

Trichothecene mycotoxins – 3D QSAR studyof the toxicity of trichothecene mycotoxins,4485

Tricyclic – Synthesis, antiviral activity, andstability of nucleoside analogs containingtricyclic bases, 3845

Tricyclic pyrimidines – Synthesis, analgesicand anti–inflammatory activities evaluationof some bi–, tri– and tetracyclic condensedpyrimidines, 4572

Triglycerides – Design, synthesis andhypolipidemic activity of novel 2–(m–toly-loxy) isobutyric acid derivatives, 2679 –Design, synthesis and hypolipidemic activi-ty of novel 2–(naphthalen–2–yloxy)propi-onic acid derivatives as desmethyl fibrateanalogs, 3973

Triorganotin(IV) dithiocarboxylates –Synthesis, spectroscopic characterization,X–ray structure and evaluation of bindingparameters of new triorganotin(IV) dithio-carboxylates with DNA, 3986

Tripentone – Synthesis of new dipyrrolo– andfuropyrrolopyrazinones related to tripen-tones and their biological evaluation aspotential kinases (CDKs1–5, GSK–3)inhibitors, 708

Tripeptidyl peptidase I – Synthesis and useo f4–peptidylhydrazido–N–hexyl–1,8–naph-thalimides as fluorogenic histochemicalsubstrates for dipeptidyl peptidase IV andtripeptidyl peptidase I, 384

Trivalent metal ions – Antimicrobial activemacrocyclic complexes of Cr(III), Mn(III)and Fe(III) with their spectroscopicapproach, 3299

Tropinones – The cytotoxic properties andpreferential toxicity to tumour cells dis-played by some2,4–bis(benzylidene)–8–methyl–8–azabicy-clo[3.2.1] octan–3–ones and 3,5–bis(ben-zylidene)–1–methyl–4–piperidones, 54

TRPV1 antagonists – Conformationally con-strained analogues of N'–(4–tert–butylben-zyl)–N–(4–methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists, 322

Trypanosoma brucei rhodesiense –Antiplasmodial and antitrypanosomal activ-ities of aminobicyclo[2.2.2]octyl�–aminoalkanoates, 736

Trypanosoma cruzi – Comparative study ofthe trypanocidal activity of the methyl1–nitrophenyl–1,2,3,4–9H–tetrahydro–�–carboline–3–carboxylate derivatives andbenznidazole using theoretical calculationsand cyclic voltammetry, 1745 – Scoringfunction for DNA–drug docking of anti-cancer and antiparasitic compounds basedon spectral moments of 2D lattice graphsformolecular dynamics trajectories, 4461 –Anti–trypanosomatid benzofuroxans anddeoxygenated analogues: Synthesis usingpolymer–supported triphenylphosphine,biological evaluation and mechanism ofaction studies, 5055

Tuberculosis – Synthesis and antimycobacte-rial activities of novel 6–nitro-quinolone–3–carboxylic acids, 345 –Synthesis, antitubercular activity and dock-ing study of novel cyclic azole substituteddiphenyl ether derivatives, 492 – Synthesis,anti–tuberculosis activity and 3D–QSARstudy of amino acid conjugates of

4–(adamantan–1–yl) group containingquinolines, 2017 – Substituted quinolinylchalcones and quinolinyl pyrimidines as anew class of anti–infective agents, 2081 – Amacrolactone from benzo[a]phenazine withpotent activity against Mycobacteriumtuberculosis, 2334 – Diversity–orientedsynthesis of furo[3,2–f]chromanes withantimycobacterial activity, 2497 – Synthesisand antitubercular screening of imidazolederivatives, 3350 – Design, synthesis andantimycobacterial activity of some novelimidazo[1,2–c]pyrimidines, 3837 –Preparation and antitubercular activities invitro and in vivo of novel Schiff bases ofisoniazid, 4169 – l–Proline–catalysed facilegreen protocol for the synthesis and antimy-cobacterial evaluation of [1,4]–thiazines,4978

Tubulin polymerization – A diaryl sulfide,sulfoxide, and sulfone bearing structuralsimilarities to combretastatin A–4, 2685

Tumor–associated isoform – Synthesis andbiological evaluation of a new family ofanti–benzylanilinosulfonamides as CA IXinhibitors, 511

Type 2 diabetes – ‘Sum of activities’ asdependent parameter: A new CoMFA–basedapproach for the design of pan PPAR ago-nists, 42

Type I DNA topoisomerase – Synthesis andbiological activity evaluation of 1H–benz-imidazoles via mammalian DNA topoiso-merase I and cytostaticity assays, 2280

Tyrosinase inhibitor – A class of potenttyrosinase inhibitors:Alkylidenethiosemicarbazide compounds,1773 – Inhibitory effects of 5–benzylidenebarbiturate derivatives on mushroom tyrosi-nase and their antibacterial activities, 4235

Tyrosinase – Dopamine– and tyramine–basedderivatives of triazenes: Activation bytyrosinase and implications for prodrugdesign, 3228

Tyrosine kinase inhibitor – Determination ofpermeability and lipophilicity ofpyrazolo–pyrimidine tyrosine kinaseinhibitors and correlation with biologicaldata, 3712

Tyrosine kinase inhibitors – Synthesis andcharacterization of rhenium and tech-netium–99m tricarbonyl complexes bearingthe 4–[3–bromophenyl]quinazoline moietyas a biomarker for EGFR–TK imaging,4021

UUlcerogenic activities – S– and C–nucleosi-

doquinazoline as new nucleoside analogswith potential analgesic and anti–inflamma-tory activity, 4249

Ulcerogenic activity – Synthesis and pharma-cological investigation of 3–(substituted1–pheny le thanone )–4–( subs t i t u t edphenyl)–1, 2, 3, 4–tetrahydropyrimi-dine–5–carboxylates, 3645

Ulcerogenic – Synthesis and pharmacologicalevaluation of 2(3H)–furanones and2(3H)–pyrrolones, combining analgesic andanti–inflammatory properties with reduced

Page 53: Chal Micro

Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184 5183

gastrointestinal toxicity and lipid peroxida-tion, 2636 – Fenbufen based 3–[5–(substi-tuted aryl)–1,3,4–oxadiazol–2–yl]–1–(biphenyl–4–yl)propan–1–ones as saferantiinflammatory and analgesic agents,3798 – Synthesis of 6–aminomethyl deriva-tives of benzopyran–4–one with dual bio-logical properties: Anti–inflammatory–anal-gesic and antimicrobial, 4896

Ultrasonic reactions – A facile synthesis ofnovel biologically active4–hydroxy–N'–(benzylidene)–2H–benzo[e][1,2]thiazine–3–carbohydrazide 1,1–diox-ides, 1311

Ultrasounds – Diazinium salts with dihydrox-yacetophenone skeleton: Syntheses andantimicrobial activity, 2275

Umbelliferone – Antiamoebic coumarins fromthe root bark of Adina cordifolia and theirnew thiosemicarbazone derivatives, 2252

Unilamellar vesicles – Physicochemical prop-erties and membrane interactions ofanti–apoptotic derivatives 2–(4–fluo-rophenyl)–3–(pyridin–4–yl)imidazo[1,2–a]pyridine depending on the hydroxyalky-lamino side chain length and conformation:An NMR and ESR study, 3509

Unsaturated dideoxy fluoro ketonucleosides– Unsaturated dideoxy fluoro–ketopyra-nosyl nucleosides as new cytostatic agents:A convenient synthesis of2,6–dideoxy–3–fluoro–4–keto–�–d–glu-copyranosyl analogues of uracil, 5–fluo-rouracil, thymine, N4–benzoyl cytosine andN6–benzoyl adenine, 4764

UO2(II) complexes – Copper(II) anduranyl(II) complexes with acylthiosemicar-bazide: Synthesis, characterization, antibac-terial activity and effects on the growth ofpromyelocytic leukemia cells HL–60, 3323

Uracil acetamide – Design, synthesis andevaluation of novel uracil acetamide deriva-tives as potential inhibitors of Plasmodiumfalciparum dUTP nucleotidohydrolase, 678

Urea derivatives – Design, synthesis andstructure–activity relationships of antipro-liferative 1,3–disubstituted urea derivatives,453

Urea – Synthesis of some urea and thioureaderivatives of3–phenyl/ethyl–2–thioxo–2,3–dihydrothia-zolo[4,5–d]pyrimidine and their antagonis-tic effects on haloperidol–induced catalepsyand oxidative stress in mice, 3889 –Hydrolytic cleavage of DNA byurea–bridged macrocyclic polyamines,5090

Ureas – Novel ureas and thioureas of15–membered azalides with antibacterialactivity against key respiratory pathogens,3459

Urine – Highly sensitive spectrofluorimetricdetermination of lomefloxacin in spikedhuman plasma, urine and pharmaceuticalpreparations, 3402

UV data – Synthesis, antibacterial and anti-convulsant evaluations of some cyclicenaminones, 967

UV/vis absorption – Studies on the interac-tion of caffeine with bovine hemoglobin,2100

UV–vis – Synthesis and characterization ofdinuclear macrocyclic cobalt(II), copper(II)and zinc(II) complexes derived from2,2,2',2'–S,S[bis(bis–N,N–2–thiobenzimida-zolyloxalato–1,2–ethane)]: DNA bindingand cleavage studies, 834

VV2 agonists – Arginine vasopressin and its

analogues – The influence of position 2modification with 3,3–diphenylalanineenantiomers. Highly potent V2 agonists,2862

Validation – Predictive QSAR modeling ofHIV reverse transcriptase inhibitor TIBOderivatives, 1509

Vascular smooth muscle – N1–Alkylated3,4–dihydropyrimidine–2(1H)–ones:Convenient one–pot selective synthesis andevaluation of their calcium channel block-ing activity, 1997

Vasodilation – Studies towards the identifica-tion of putative bioactive conformation ofpotent vasodilator arylidene N–acylhydra-zone derivatives, 4004

Vasodilatory activity – Synthesis andvasodilatory activity of some amide deriva-tives of 6–(4–carboxymethy-loxyphenyl)–4,5–dihydro–3(2H)–pyridazi-none, 4441

Vasodilatory – Design, synthesis and pharma-cological screening of novel nitric oxidedonors containing1,5–diarylpyrazolin–3–one as nontoxicNSAIDs, 4622

VEGF–R – Design, synthesis and characteri-zation of N9/N7–substituted 6–aminopurinesas VEGF–R and EGF–R inhibitors, 1788

Veratric acid – Hansch analysis of veratricacid derivatives as antimicrobial agents, 689

Virtual library design – Design and in silicoscreening of combinatorial library of anti-malarial analogs of triclosan inhibitingPlasmodium falciparum enoyl–acyl carrierprotein reductase, 3009

Virtual library screening – Fragment andknowledge–based design of selectiveGSK–3� inhibitors using virtual screeningmodels, 2361

Virtual ligand screening – MED–3DMC: Anew tool to generate 3D conformation ensem-bles of small molecules with a Monte Carlosampling of the conformational space, 1405

Virtual screening – Virtual screening forRaf–1 kinase inhibitors based on pharma-cophore model of substituted ureas, 1240 –Structure–based virtual screening approachto identify novel classes of PTP1Binhibitors, 3280 – Important pharmacophor-ic features of pan PPAR agonists: Commonchemical feature analysis and virtualscreening, 3488 – Discovery of potentialnew InhA direct inhibitors based on phar-macophoreand 3D–QSAR analysis fol-lowed by in silico screening, 3718 – An effi-cient steroid pharmacophore–based strategyto identify new aromatase inhibitors, 4121 –Pharmacophore modeling and virtualscreening for the discovery of new trans-forming growth factor–� type I receptor

(ALK5) inhibitors, 4259 – Discovery ofpotential ZAP–70 kinase inhibitors:Pharmacophore design, database screeningand docking studies, 4793

Voltage–gated potassium channel –4–Phenoxybutoxy–substituted heterocycles– A structure–activity relationship study ofblockers of the lymphocyte potassium chan-nel Kv1.3, 1838

Voltammetry – New insights into the antioxi-dant activity of hydroxycinnamic acids:Synthesis and physicochemical characteri-zation of novel halogenated derivatives,2092

Volume of distribution – Prediction of vol-ume of distribution values in human usingimmobilized artificial membrane partition-ing coefficients, the fraction of compoundionized and plasma protein binding data,4455

WWake promoting – Diamine–based human

histamine H3 receptor antagonists:(4–Aminobutyn–1–yl)benzylamines, 4098

Wang–Ford charges – QSAR modelling ofpancreatic �–cell KATP channel openersR/S–3,4–dihydro–2,2–dimethyl–6–halo–4–( s u b s t i t u t e dphenylaminocarbonylamino)–2H–1–ben-zopyrans using MLR–FA techniques, 359

Wasabi – Anti–nitric oxide production activi-ty of isothiocyanates correlates with theirpolar surface area rather than theirlipophilicity, 4931

Wee1 kinase inhibitor – Receptor–based3D–QSAR studies of checkpoint Wee1kinase inhibitors, 1383

WEKA – Development of QSAR models forpredicting hepatocarcinogenic toxicity ofchemicals, 3658

Wine – QSAR study of antioxidant activity ofwine polyphenols, 400

Wittig–Horner carbanions – Application ofphosphonyl carbanions to highly regioselec-tive synthesis of some diazaphospholes andpyrazolinyl phosphonates, 526

Wittig–Horner reaction – Synthesis of noveltrans–stilbene derivatives and evaluation oftheir potent antioxidant and neuroprotectiveeffects, 3166

Wound healing activity – Synthesis of novelbenzo[h]quinolines: Wound healing, anti-bacterial, DNA binding and in vitro antiox-idant activity, 981

Wound healing – Evaluation of in vivowound–healing potential of2–[4–(2,4–dimethoxy–benzoyl)–phe-noxy]–1–[4–(3–piperidin–4–yl–propyl)–piperidin–1–yl]–ethanone derivatives, 3158

Writhing test – Synthesis and antinociceptiveactivities of some pyrazoline derivatives,2606

XXanthones – Bromoalkoxyxanthones as

promising antitumor agents: Synthesis,crystal structure and effect on human tumorcell lines, 3830

Page 54: Chal Micro

5184 Keyword index / European Journal of Medicinal Chemistry 44 (2009) 5131–5184

Xanthotoxin – Synthesis and antitumor activityof some new xanthotoxin derivatives, 2967

XDR–tuberculosis (TB) – Pentacyclo–unde-cane derived cyclic tetra–amines: Synthesisand evaluation as potent anti–tuberculosisagents, 4297

X–ray analysis – Design of novel aminopy-rrolidine factor Xa inhibitors from a screen-ing hit, 2787

X–ray crystal structure analysis – Synthesis,structure elucidation and antitumour activi-ty of N–substituted amides of 3–(3–ethyl-thio–1,2,4–triazol–5–yl)propenoic acid,3788 – Synthesis, pharmacological andantiviral activity of 1,3–thiazepine deriva-tives, 4960

X–ray crystallography – The cytotoxic prop-erties and preferential toxicity to tumourcells displayed by some 2,4–bis(benzyli-dene)–8–methyl–8–azabicyclo[3.2.1]octan–3–ones and 3,5–bis(benzyli-dene)–1–methyl–4–piperidones, 54 –Synthesis of new chiral 2,5–disubstituted1,3,4–thiadiazoles possessing �–butenolidemoiety and preliminary evaluation of invitro anticancer activity, 3340 – Antiviralevaluation of N–amino–1,2,3–triazolesagainst Cantagalo virus replication in cellculture, 3777 – Stereoselective synthesisand antimicrobial activity ofbenzofuran–based (1E)–1–(piperidin–1–yl)–N2–arylamidrazones, 4985 – Crystal struc-tures, antioxidation and DNA binding prop-erties of Dy(III) complexes withSchiff–base ligands derived from 8–hydrox-

yquinoline–2–carboxaldehyde and fouraroylhydrazines, 5080

X–ray diffraction – Synthesis, crystal struc-ture and anti–inflammatory properties ofcurcumin analogues, 915 –Bromoalkoxyxanthones as promising anti-tumor agents: Synthesis, crystal structureand effect on human tumor cell lines, 3830– Synthesis, spectroscopic characterization,X–ray structure and evaluation of bindingparameters of new triorganotin(IV) dithio-carboxylates with DNA, 3986 – Novel3,3'–diindolylmethane derivatives:Synthesis and cytotoxicity, structural char-acterization in solid state, 4136

X–ray – Novel trans–dichloridoplatinum(II)complexes with 3– and 4–acetylpyridine:Synthesis, characterization, DFT calcula-tions and cytotoxicity, 1921 – Synthesis andstructure analysis of cyclodehydration prod-uct of piroxicam: A metabolite detected indogs and monkeys, 3368 – Synthesis, crys-tal structures and antibacterial activity stud-ies of aza–derivatives of phytoalexin fromcotton plant – gossypol, 4393

X–ray single crystal – Convenient synthesisand antimicrobial evaluation of some novel2–substituted–3–methylbenzofuran deriva-tives, 3637

X–ray structure – The structure ofRimonabant in the solid state and in solu-tion: An experimental and theoretical study,1864

X–ray study – Synthesis of novel thia-zolone–based compounds containing pyra-

zoline moiety and evaluation of their anti-cancer activity, 1396

Xylene derivatives – Synthesis and antiproto-zoal activities of dicationic bis(phe-noxymethyl)benzenes, bis(phe-noxymethyl)naphthalenes, and bis(benzy-loxy)naphthalenes, 3543

Xylene linkers – In–vitro regeneration ofsarin inhibited electric eel acetyl-cholinesterase by bis–pyridinium oximesbearing xylene linker, 1326

YYeast cultures – Synthesis, Raman, FT–IR,

NMR spectroscopic characterization,antimicrobial activity, cytotoxicity andDNA binding of new mixed aza–oxo–thiamacrocyclic compounds, 4681

Ylidenemalononitriles – Synthesis of[1,2,4]triazolo[1,5–a]pyridines of potentialPGE2 inhibitory properties, 1972

ZZAP–70 – Discovery of potential ZAP–70

kinase inhibitors: Pharmacophore design,database screening and docking studies, 4793

Zileuton – Synthesis and pharmacologicalevaluation of 2–substituted benzo[b]thio-phenes as anti–inflammatory and analgesicagents, 1718

Zn(II) complex – Synthesis and characteriza-tion of the Zn(II) and Cu(II) piperidinylisoeuxanthone complexes: DNA–bindingand cytotoxic activity, 4509