Abstract
A series of novel 1,2,4-triazole thioacetanilide derivatives has been designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. Half of these compounds showed moderate to potent activities against wild-type HIV-1 with an EC50 ranging from 38.0 μM to 4.08 µM. Among them, 2-(4-(2-fluorobenzyl)-5-isopropyl-4H-1,2,4-triazol- 3-ylthio)-N-(2-nitrophenyl)acetamide 7d was identified as the most promising compound (EC50 = 4.26 µM, SI = 49). However, no compound was active against HIV-2. The preliminary structure-activity relationships among the newly synthesized congeners are 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* / pharmacology
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Cells, Cultured
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Drug Design
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Enzyme Activation / drug effects
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Humans
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology*
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology
Substances
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Acetanilides
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Anti-HIV Agents
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Reverse Transcriptase Inhibitors
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Triazoles
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1,2,4-triazole
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thioacetanilide