Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Bioorg Med Chem Lett. 2006 Feb;16(3):668-71. doi: 10.1016/j.bmcl.2005.10.037. Epub 2005 Nov 17.

Abstract

Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het=2-thiazoyl and 2-pyrimidinyl are the focus of this report.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amines / chemistry*
  • Amines / pharmacology
  • Drug Resistance, Multiple, Viral
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • Heterocyclic Compounds / chemistry
  • Hydrophobic and Hydrophilic Interactions
  • Pyrimidines / chemistry
  • Reverse Transcriptase Inhibitors / chemical synthesis*
  • Reverse Transcriptase Inhibitors / pharmacology
  • Structure-Activity Relationship
  • Thiazoles / chemistry

Substances

  • Amines
  • Heterocyclic Compounds
  • Pyrimidines
  • Reverse Transcriptase Inhibitors
  • Thiazoles
  • HIV Reverse Transcriptase