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

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

Volume: 9 Issue: 7

Author(s): Zhenyu Li, Yuan Cao, Peng Zhan, Christophe Pannecouque, Jan Balzarini, Erik De Clercq, Yuemao Shen and Xinyong Liu

Affiliation:

Keywords: HIV-1, AIDS, NNRTIs, 1, 2, 4-triazole thioacetanilides, Anti-HIV-1 activity.

Abstract: 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 μM to 4.08 µM. 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 µM, SI = 49). However, no compound was active against HIV-2. The preliminary structure-activity relationships among the newly synthesized congeners are discussed.

Cite this article as:

Li Zhenyu, Cao Yuan, Zhan Peng, Pannecouque Christophe, Balzarini Jan, Clercq De Erik, Shen Yuemao and Liu Xinyong, Arylazolylthioacetanilide. Part 11: Design, Synthesis and Biological Evaluation of 1,2,4-triazole Thioacetanilide Derivatives as Novel Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070010