Styrylquinazoline derivatives as HIV-1 integrase inhibitors

Arch Pharm (Weinheim). 2002 Jun;335(6):277-82. doi: 10.1002/1521-4184(200208)335:6<277::AID-ARDP277>3.0.CO;2-A.

Abstract

Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50) = 130.7 +/- 8.6 microM).

MeSH terms

  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacology*
  • HIV-1 / enzymology*
  • Humans
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Oligonucleotides / chemistry
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology*
  • Structure-Activity Relationship

Substances

  • HIV Integrase Inhibitors
  • Indicators and Reagents
  • Oligonucleotides
  • Quinazolines