SYNOPSIS OF THE THESIS TO BE SUBMITTED TO

BHAVNAGAR UNIVERSITY FOR Ph.D. DEGREE IN

CHEMISTRY

FACULTY : SCIENCE

TITLE : BIO-ACTIVE HETEROCYCLIC

COMPOUNDS AS

POTENTIAL ANTIMICROBIAL AGENTS

NAME OF THE CANDIDATE : SHIHORA PRASHANT NANUBHAI

NAME OF THE GUIDE : PROF. NISHEETH C. DESAI

REGISTRATION NUMBER : 963

DATE OF REGISTRATION : 16/04/2005

PLACE OF WORK : DEPARTMENT OF CHEMISTRY,

BHAVNAGAR UNIVERSITY,

BHAVNAGAR-364 002,

(INDIA)

BIO-ACTIVE HETEROCYCLIC COMPOUNDS AS POTENTIAL ANTIMICROBIAL AGENTS

Medicinal and bio-organic chemistry is concerned with the

design, synthesis, and analysis of the relationship between

molecular structure and biological activity for compounds that

can be used for the cure or treatment of disease. Heterocyclic

chemistry is fundamental to biology and medicine. It is not

farfetched to say that we are living in the age of Heterocyclic

chemistry. The emergence of drug resistant bacteria has posed a

growing challenge to the search for new chemical entities. Yet,

from the viewpoint of drug discovery it is critical to realize that,

despite the importance of drug knowledge, it is not an exclusive

tool. Rather, it is a tool that must be used with the techniques of

combinatorial chemistry, structural biology, high throughput

screening, siRNA, in silico design & related technologies.

The dynamics of drug development is one of the defining

characteristics of pharmaceutical industry. Despite its importance

to industry, there is little information on how long it takes for

particular drugs to go through human clinical trials and the

probabilities of successful completion.

Useful drugs like risperidone, pyrethrin, isoniazide, rotenone,

AZT, strychnine, reserpine, some antihistamines, ergot alkaloids,

caffeine, cocaine and barbiturates are heterocyclic compounds.

Recently some non-nucleoside heterocyclic compounds like

nivirapine, TIBO, BHAP, PETT and HEPT have been used as anti-

HIV agents. The latest anticancer drug is Fludarabine, which

contain heterocyclic framework in the structure. Looking to the

importance of heterocyclic compounds in medicinal chemistry, we

have synthesized the following heterocyclic compounds and

screened for their in vitro antimicrobial activity.

Heterocyclic compounds like 4-oxo-quinazoline, 4-oxo-

thiazolidin, 5-oxo-imidazole, 1,2,4-triazol and their derivatives

have been found to possess strong hypnotic, anaesthetic,

analgesic, sedative, antifungal, antitubercular, anticonvulsant,

CNS-depressant, anti-HIV, anticancer and antibacterial activities.

Part-I

Section 1: N-{5-[(aryl)methylene]-2-(2-hydroxyphenyl]-4-

oxo(1,3-thiazolidin-3-yl)}{4-[2-(4-methylphenyl)-4-

oxo(3-hydro quinazolin-3-yl)] phenyl}carboxamides.

Section 2:N-{5-[(aryl)methylene]-2-(4-hydroxyphenyl]-4-oxo(1,3-

thiazolidin-3-yl)}{4-[2-(4-methylphenyl)-4-oxo(3-hydro

quinazolin-3-yl)]phenyl}carboxamides.

Section 3:N-{5-[(aryl)methylene]-2-(4-fluorophenyl]-4-oxo(1,3-

thiazolidin-3-yl)}{4-[2-(4-methylphenyl)-4-oxo(3-hydro

quinazolin-3-yl)]phenyl}carboxamides.

Section 4:N-{5-[(aryl)methylene]-2-(4-chlorophenyl]-4-oxo(1,3-

thiazolidin-3-yl)}{4-[2-(4-methylphenyl)-4-oxo(3-hydro

quinazolin-3-yl)]phenyl}carboxamides.

Part-II

Section 5:N-{4-[(aryl)methylene]-5-oxo-2-phenyl(2-imidazolinyl)}

{4-[2-(3-nitrophenyl)-4-oxo(3-hydroquinazolin-3-

yl)]phenyl} carboxamides.

Section 6: N-{4-[(aryl)methylene]-5-oxo-2-phenyl(2-

imidazolinyl)} {4-[2-(4-nitrophenyl)-4-oxo(3-

hydroquinazolin-3-yl)]phenyl} carboxamides.

Section 7: N-{4-[(aryl)methylene]-5-oxo-2-phenyl(2-

imidazolinyl)}-2-(1-phenyl(3H-1,2,4-triazol-3-

yloxy))acetamides.

Section 8: {4-[(Diethoxythioxophosphino)amino]phenyl}-n-

{4-[(aryl) methylene]-5-oxo-2-phenyl(2-

imidazolinyl)}carboxamides.

Part-III

Section 9: Phenyl-N-{5-naphthal-3-sulfanyl(1,2,4-triazol-4-

yl)} carboxamides.

Section 10: Phenyl-N-{5-[(4-chlorophenoxy)methyl]-3-

sulfanyl(1,2,4-triazol-4-yl)}carboxamides.

Section 11: Phenyl–N–{5–(2–naphthyloxyacetyl)-3–

sulfanyl(1,2,4–triazole-

4-yl)}carboxamides.

Section 12: Phenyl–N–{5–[(3-nitrophenyl)methyl]–3–

sulfanyl(1,2,4–triazole-4-yl)}carboxamides.

Part-I : Structures of the synthesized compounds

Section : 1 Section : 2

Section : 3 Section : 4

Where Ar = Different aryl group

Part-II : Structures of the synthesized compounds

Section : 5 Section : 6

Section : 7 Section : 8

Where Ar = Different aryl group

Part-III : Structures of the synthesized compounds

Section : 9 Section :10

Section : 11 Section : 12

Where Ar = Different aryl groupPart-IV: Biological evaluation and characterization

The study in part four is divided into following two sections.

Section A: This section deals with the biological evaluation of

the compounds synthesised in part I, II and III.

Section B: In this section we will discuss the spectroscopic

analysis of the compounds reported in part I, II and III.

Signature of the guide Signature of the

candidate

Prof. Nisheeth C. Desai Shihora Prashant Nanubhai

Date: 29/06/2007

Place: BHAVNAGAR