Bioorganic & Medicinal Chemistry 2009-08-15

Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Peng Zhan, Xinyong Liu, Junjie Zhu, Zengjun Fang, Zhenyu Li, Christophe Pannecouque, Erik De Clercq

Index: Bioorg. Med. Chem. 17(16) , 5775-81, (2009)

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Abstract

A series of 2-(1-aryl-1H-imidazol-2-ylthio)acetamide [imidazole thioacetanilide (ITA)] derivatives were synthesized and evaluated as potent inhibitors of human immunodeficiency virus type-1 (HIV-1). Among them, the most potent HIV-1 inhibitors were 4a5 (EC(50)=0.18microM), and 4a2 (EC(50)=0.20microM), which were more effective than the lead compound L1 (EC(50)=2.053microM) and the reference drugs nevirapine and delavirdine. The preliminary structure-activity relationship (SAR) of the newly synthesized congeners is discussed.