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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetanilides / chemical synthesis*
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Acetanilides / chemistry
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Acetanilides / pharmacology
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology
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Binding Sites
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Computer Simulation
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV Reverse Transcriptase / metabolism
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Humans
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Imidazoles / chemical synthesis
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Imidazoles / chemistry*
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Imidazoles / pharmacology
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Structure-Activity Relationship
Substances
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Acetanilides
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Anti-HIV Agents
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Imidazoles
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reverse transcriptase, Human immunodeficiency virus 1
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HIV Reverse Transcriptase
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thioacetanilide