Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase

被引：109

作者：

De La Rosa, Martha ^{[1
]}

Kim, Hong Woo ^{[1
]}

Gunic, Esmir ^{[1
]}

Jenket, Cheryl ^{[1
]}

Boyle, Uyen ^{[1
]}

Koh, Yung-hyo ^{[1
]}

Korboukh, Ilia ^{[1
]}

Allan, Matthew ^{[1
]}

Zhang, Weijian ^{[1
]}

Chen, Huanming ^{[1
]}

Xu, Wen ^{[1
]}

Nilar, Shahul ^{[1
]}

Yao, Nanhua ^{[1
]}

Hamatake, Robert ^{[1
]}

Lang, Stanley A. ^{[1
]}

Hong, Zhi ^{[1
]}

Zhang, Zhijun ^{[1
]}

Girardet, Jean-Luc ^{[1
]}

机构：

[1] Valeant Res & Dev, Costa Mesa, CA 92626 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 17期

关键词：

antiviral; HIV-1; NNRTI; triazole; K103N; Y181C; Y188L;

D O I：

10.1016/j.bmcl.2006.06.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthio-semicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4444 / 4449

页数：6

共 12 条

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