Abstract
The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.
MeSH terms
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Anti-HIV Agents / chemistry*
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Anti-HIV Agents / pharmacology*
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Drug Evaluation, Preclinical
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HIV Reverse Transcriptase / antagonists & inhibitors
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HIV Reverse Transcriptase / drug effects
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HIV Reverse Transcriptase / genetics
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HIV-1 / drug effects
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HIV-1 / genetics
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Inhibitory Concentration 50
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Mutation
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Nitriles / chemistry*
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Nitriles / pharmacology*
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology*
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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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6-amino-5-bromo-4-(4-cyano-2,6-dimethylphenoxy)-2-(4-cyanophenylamino)pyrimidine
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Anti-HIV Agents
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Nitriles
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Pyrimidines
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Reverse Transcriptase Inhibitors
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HIV Reverse Transcriptase