A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2169-72. doi: 10.1016/s0960-894x(98)00369-2.

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

  • Amino Acid Substitution
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Drug Design
  • HIV Reverse Transcriptase / chemistry
  • HIV Reverse Transcriptase / metabolism*
  • Humans
  • Kinetics
  • Molecular Structure
  • Mutagenesis, Site-Directed
  • Nevirapine / analogs & derivatives*
  • Nevirapine / chemical synthesis
  • Nevirapine / chemistry*
  • Nevirapine / pharmacology
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Reverse Transcriptase Inhibitors / chemical synthesis*
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • Pyridines
  • Recombinant Proteins
  • Reverse Transcriptase Inhibitors
  • Nevirapine
  • HIV Reverse Transcriptase