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Letters in Drug Design & Discovery

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

DOI: 10.2174/1570180811309010027

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Synthesis and Anti-HIV Evaluation of Novel 1,2,4-triazole Derivatives as Potential Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors

Page: [27 - 34] Pages: 8

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Abstract

A series of novel 1,2,4-triazole derivatives has been designed and synthesized. All of the new compounds were evaluated for their anti-HIV activities in MT-4 cells. Three of them showed moderate activities against wild-type HIV-1 with an EC50 ranging from 17.4 μM to 4.87 μM. Among the active compounds, 3-((4-(3,4-dimethoxybenzylideneamino)- 5-(furan-2-yl)-4H-1,2,4-triazol-3-ylthio)methyl)benzonitrile (4d) was identified as the promising compound (EC50 = 17.4 μM, SI =13). However, no compound displayed inhibitory activity against HIV-2.

Keywords: HIV-1, AIDS, NNRTIs, Triazoles, Synthesis, Anti-HIV-1 activity, NNRTIs, LC Autosampler Device, heterocyclic scaffold, Nexus 470FT-IR