1, 2, 3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors

P Zhan, X Liu, Y Cao, Y Wang, C Pannecouque…

Index: Zhan, Peng; Liu, Xinyong; Cao, Yuan; Wang, Yan; Pannecouque, Christophe; De Clercq, Erik Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5368 - 5371

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Citation Number: 67

Abstract

A novel series of 1, 2, 3-thiadiazole thioacetanilide (TTA) derivatives have been designed, synthesized and evaluated for its anti-HIV activities in MT-4 cells. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations. Among them, 2-[4-(2, 4-dichlorophenyl)-1, 2, 3-thiadiazol-5-ylthio]-N-(2-nitrophenyl) acetamide 7d2 was identified as the most promising compound (EC50= 0.059±0.02 μM, CC50> 283.25 ...

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