Arylazolylthioacetanilide. Part 11: Design, Synthesis and Biological Evaluation of 1,2,4-triazole Thioacetanilide Derivatives as Novel Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors

被引：12

作者：

Li, Zhenyu ^{[1
]}

Cao, Yuan ^{[1
]}

Zhan, Peng ^{[1
]}

Pannecouque, Christophe ^{[2
]}

Balzarini, Jan ^{[2
]}

De Clercq, Erik ^{[2
]}

Shen, Yuemao ^{[1
]}

Liu, Xinyong ^{[1
]}

机构：

[1] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, Jinan 250012, Peoples R China

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

来源：

MEDICINAL CHEMISTRY | 2013年 / 9卷 / 07期

基金：

中国国家自然科学基金; 高等学校博士学科点专项科研基金;

关键词：

HIV-1; AIDS; NNRTIs; 1,2,4-triazole thioacetanilides; Anti-HIV-1; activity;

D O I：

10.2174/1573406411309070010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 1,2,4-triazole thioacetanilide derivatives has been designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. Half of these compounds showed moderate to potent activities against wild-type HIV- 1 with an EC50 ranging from 38.0 mu M to 4.08 mu M. Among them, 2-(4-(2- fluorobenzyl)-5-isopropyl-4H-1,2,4-triazol-3-ylthio)-N-(2- nitrophenyl) acetamide 7d was identified as the most promising compound ( EC50 = 4.26 mu M, SI = 49). However, no compound was active against HIV-2. The preliminary structure-activity relationships among the newly synthesized congeners are discussed.

引用

页码：968 / 973

页数：6

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