Abstract
A series of 4,4-disubstituted quinolinones was prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The C-3 substituted compound 9h displayed improved antiviral activity against clinically significant single (K103N) and double (K103N/L100I) mutant viruses.
MeSH terms
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Antiviral Agents / chemical synthesis
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Antiviral Agents / pharmacology*
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Drug Resistance / genetics
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV-1 / drug effects*
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HIV-1 / genetics
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Humans
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Inhibitory Concentration 50
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Mutation / genetics
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Quinolones / chemical synthesis
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Quinolones / pharmacology*
Substances
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Antiviral Agents
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Quinolones
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HIV Reverse Transcriptase