Abstract
The syntheses of 11-ethyl and 11-cyclopropyldipyrido[2,3-b:3',2'-f]azepines, analogs of the HIV-1 reverse transcriptase inhibitor nevirapine 1, are described. These compounds exhibit potency equivalent to nevirapine in the inhibition of wild-type and some mutant RT enzymes.
MeSH terms
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Amino Acid Substitution
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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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Drug Design
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HIV Reverse Transcriptase / chemistry
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HIV Reverse Transcriptase / metabolism*
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Humans
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Kinetics
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Molecular Structure
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Mutagenesis, Site-Directed
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Nevirapine / analogs & derivatives*
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Nevirapine / chemical synthesis
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Nevirapine / chemistry*
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Nevirapine / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Recombinant Proteins / chemistry
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Recombinant Proteins / metabolism
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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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Anti-HIV Agents
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Pyridines
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Recombinant Proteins
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Reverse Transcriptase Inhibitors
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Nevirapine
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HIV Reverse Transcriptase