Synthesis and HIV integrase inhibitory activity of caffeic acid derivatives

Aim To synthesize a series of new caffeic acid derivatives and test their HIV-1 integrase inhibitory activities.Methods A series of N-substituted caffeoyl-naphthalenesulfonaminde derivatives were synthesized by six-step reactions.HIV-1 integrase inhibitory assay of these compounds was carried out by ()~(32)P-marked experiments in vitro.Resluts Twenty caffeic acid derivatives were synthesized and confirmed by IR,()~1H-NMR and MS.Among these compounds,the HIV-1 integrase inhibitory activities of compounds Ⅰ_2,Ⅰ_3 and Ⅰ_4 were more potent than that of L-chicoric acid(IC_(50)=11.8 μg ·mL~(-1)).Conclusion N-substituted caffeoyl-naphthalenesulfonaminde derivatives show remarkable HIV-1 integrase inhibitory activities,and further research is underway.