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Bioorg Med Chem. 2009 Aug 15;17(16):5775-81. doi: 10.1016/j.bmc.2009.07.028. Epub 2009 Jul 18.

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

Author information

1
Institute of Medicinal Chemistry, Shandong University, Jinan, PR China.

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.

PMID:
19643613
DOI:
10.1016/j.bmc.2009.07.028
[Indexed for MEDLINE]

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