Styrylquinazoline derivatives as HIV-1 integrase inhibitors

Abstract

Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5 c containing a free catechol ring was the most potent (IC50 = 20.8 +/- 1.9 muM) and showed 6-fold more potency than the corresponding styrylquinoline compound (IC50 = 130.7+/-8.6 muM).