Synthesis and Biological Evaluation of a New Series of 2-{[4-(3,4-Dichlorophenyl)-1,2,3-thiadiazol-5-yl]sulfanyl}acetanilides as HIV-1 Inhibitors

被引：28

作者：

Zhan, Peng ^{[1
]}

Liu, Xin-Yong ^{[1
]}

Li, Zhen-Yu ^{[1
]}

Fang, Zeng-Jun ^{[1
]}

Pannecouque, Christophe ^{[2
]}

De Clereq, Erik ^{[2
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Inst Med Chem, Jinan 250012, Peoples R China

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

CHEMISTRY & BIODIVERSITY | 2010年 / 7卷 / 07期

关键词：

REVERSE-TRANSCRIPTASE INHIBITORS; POTENT NONNUCLEOSIDE INHIBITORS; COLORIMETRIC ASSAY; DESIGN; NNRTIS; THIOACETANILIDES; CHEMOTHERAPY; FUTURE; MUTANT; DRUGS;

D O I：

10.1002/cbdv.200900197

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

As part of our studies to discover new HIV-1 reverse transcriptase inhibitors, a series of 3,4-dichlorophenyl substituted 1,2,3-thiadiazole thioacetanilide (TTA = [ (1,2,3-thiadiazole-5-yl)sulfanyl acet anilide) derivatives were synthesized, and in vitro anti-HIV activity was evaluated. The results revealed that nearly half of the compounds show moderate-to-good inhibitory potency against HIV-1. In particular, compound 7f is highly potent, with an EC50 value of 0.95+/-0.33 mu M. The preliminary structure - activity relationship among the newly synthesized congeners is discussed.

引用

页码：1717 / 1727

页数：11

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