Styrylquinazoline derivatives as HIV-1 integrase inhibitors

Article abstract of DOI:10.1002/1521-4184(200208)335:6<277::AID-ARDP277>3.0.CO;2-A

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 μM) and showed 6-fold more potency than the corresponding styrylquinoline compound (IC₅₀ = 130.7 ± 8.6 μM).