ChemInform Abstract: Nonnucleoside Human Cytomegalovirus Inhibitors: Synthesis and Antiviral...

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2000 thiadiazine derivatives thiadiazine derivatives R 0660 50 - 172 Nonnucleoside Human Cytomegalovirus Inhibitors: Synthesis and Antiviral Evaluation of (Chlorophenylmethyl)benzothiadiazine Dioxide Derivatives. Among a new series of chlorophenylmethyl benzothiadiazine dioxide derivatives, e.g. (I) and (II), evaluated for their activity against human cytomegalovirus (HCMV), derivatives (Ia)–(Id) emerge as the most active HCMV inhibitors with similar selectivity, whereas compound (IIa) shows only slight antivirus activity and derivatives (Ie), (IIb), and (IIc) are totally inactive. The antiviral activity of derivative (Ia) against a variety of HCMV clinical isolates from patients with different clinical manifestations and against a ganciclovir-resistant strain confirms the hypothesis that this new series exerts antiviral action by a biological mechanism different from that of ganciclovir. — (MARTINEZ, ANA; GIL, CARMEN; PEREZ, CONCEPCION; CASTRO, ANA; PRIETO, COLUMBIANA; OTERO, JOAQUIN; ANDREI, GRACIELA; SNOECK, ROBERT; BALZARINI, JAN; DE CLERCQ, ERIK; J. Med. Chem. 43 (2000) 17, 3267-3273; Inst. Quim. Med., CSIC, E-28006 Madrid, Spain; EN) 1

Transcript of ChemInform Abstract: Nonnucleoside Human Cytomegalovirus Inhibitors: Synthesis and Antiviral...

2000 thiadiazine derivatives

thiadiazine derivativesR 0660

50 - 172Nonnucleoside Human Cytomegalovirus Inhibitors: Synthesis andAntiviral Evaluation of (Chlorophenylmethyl)benzothiadiazineDioxide Derivatives. — Among a new series of chlorophenylmethylbenzothiadiazine dioxide derivatives, e.g. (I) and (II), evaluated for theiractivity against human cytomegalovirus (HCMV), derivatives (Ia)–(Id) emergeas the most active HCMV inhibitors with similar selectivity, whereas compound(IIa) shows only slight antivirus activity and derivatives (Ie), (IIb), and (IIc)are totally inactive. The antiviral activity of derivative (Ia) against a varietyof HCMV clinical isolates from patients with different clinical manifestationsand against a ganciclovir-resistant strain confirms the hypothesis that this newseries exerts antiviral action by a biological mechanism different from that ofganciclovir. — (MARTINEZ, ANA; GIL, CARMEN; PEREZ, CONCEPCION;CASTRO, ANA; PRIETO, COLUMBIANA; OTERO, JOAQUIN; ANDREI,GRACIELA; SNOECK, ROBERT; BALZARINI, JAN; DE CLERCQ, ERIK;J. Med. Chem. 43 (2000) 17, 3267-3273; Inst. Quim. Med., CSIC, E-28006Madrid, Spain; EN)

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