Abstract
A new series of 1,2,4-triazoles was synthesized and tested against several NNRTI-resistant HIV-1 isolates. Several of these compounds exhibited potent antiviral activities against efavirenz- and nevirapine-resistant viruses, containing K103N and/or Y181C mutations or Y188L mutation. Triazoles were first synthesized from commercially available substituted phenylthiosemicarbazides, then from isothiocyanates, and later by condensing the desired substituted anilines with thiosemicarbazones.
MeSH terms
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV Reverse Transcriptase / metabolism
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HIV-1 / drug effects
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HIV-1 / enzymology
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Molecular Structure
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Nucleosides / chemical synthesis
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Nucleosides / chemistry
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Nucleosides / 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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Enzyme Inhibitors
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Nucleosides
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Triazoles
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HIV Reverse Transcriptase