Abstract
Two series of benzoxazinones differing in the aromatic substitution pattern were prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The 5-fluoro (5a-d) and 6-nitro (5e-h) substituted compounds displayed activity comparable or better than Efavirenz, the lead structure of the series.
MeSH terms
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Alkynes
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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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Benzoxazines
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Cyclopropanes
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Drug Evaluation, Preclinical
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HIV Reverse Transcriptase / drug effects
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Oxazines / chemical synthesis*
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Oxazines / chemistry*
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Oxazines / pharmacology
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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
Substances
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Alkynes
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Anti-HIV Agents
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Benzoxazines
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Cyclopropanes
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Oxazines
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Reverse Transcriptase Inhibitors
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HIV Reverse Transcriptase
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efavirenz