Synthesis and anti-HIV evaluation of the novel 2-(m-chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines

Ren-Zhang Yan; Xin-Yong Liu; Wen-Fang Xu; Christophe Pannecouque; Myriam Witvrouw; Erik De Clercq

doi:10.1007/BF02969278

Synthesis and anti-HIV evaluation of the novel 2-(m-chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines

Arch Pharm Res. 2006 Nov;29(11):957-62. doi: 10.1007/BF02969278.

Authors

Ren-Zhang Yan¹, Xin-Yong Liu, Wen-Fang Xu, Christophe Pannecouque, Myriam Witvrouw, Erik De Clercq

Affiliation

¹ Institute of Medicinal Chemistry, School of Pharmacy, Shandong University, 250012 Jinan, China.

PMID: 17146963
DOI: 10.1007/BF02969278

Abstract

A novel series of 2-(m-Chlorobenzyl)-4-substituted-1, 1, 3-trioxo-2H, 4H-pyrazolo[4, 5-e][1, 2, 4] thiadiazines (7a-k) were synthesized, and evaluated for their anti-HIV replication in MT-4 cell cultures. Compound (7a) showed activity against HIV-1-induced cytopathicity, with an EC50 value of 45.6 microM, but none of the compounds exhibited inhibitory activity against HIV-2.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / pharmacology*
Cell Line
Cytopathogenic Effect, Viral / drug effects
Drug Design
HIV-1 / drug effects
HIV-2 / drug effects
Humans
Pyrazoles / chemical synthesis*
Pyrazoles / pharmacology*
Structure-Activity Relationship
Thiadiazines / chemical synthesis*
Thiadiazines / pharmacology*

Substances

Anti-HIV Agents
Pyrazoles
Thiadiazines