Synthesis and HIV-1 reverse transcriptase inhibitory activity of 3,4-disubstituted coumarin derivatives

Benzo 6-membered heterocyclic compounds are important reverse transcriptase inhibitors.Active compounds reported in the literature have a hydrophobic benzene ring and an amide moiety connected with the benzene ring.Aiming at structural modification of amide part, a series of 3，4-disubstituted coumarin compounds were prepared.Their structures were confirmed by IR，MS，¹H NMR and element analysis.The results of the preliminary pharmacological test showed that seven out of twenty-three compounds possessed diverse HIV-1 reverse transcriptase inhibitory activity.