Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2235-9. doi: 10.1016/s0960-894x(01)00412-7.

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

  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology*
  • Drug Evaluation, Preclinical
  • HIV Reverse Transcriptase / antagonists & inhibitors
  • HIV Reverse Transcriptase / drug effects
  • HIV Reverse Transcriptase / genetics
  • HIV-1 / drug effects
  • HIV-1 / genetics
  • Inhibitory Concentration 50
  • Mutation
  • Nitriles / chemistry*
  • Nitriles / pharmacology*
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology*
  • Reverse Transcriptase Inhibitors / chemistry
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship

Substances

  • 6-amino-5-bromo-4-(4-cyano-2,6-dimethylphenoxy)-2-(4-cyanophenylamino)pyrimidine
  • Anti-HIV Agents
  • Nitriles
  • Pyrimidines
  • Reverse Transcriptase Inhibitors
  • HIV Reverse Transcriptase