Synthesis and HIV-1 integrase inhibition of novel bis- or tetra-coumarin analogues

Abstract

Present studies were undertaken on the preparation of synthetic analogues of bis- or tetra-coumarins and their activity against HIV-1 integrase (HIV-1 IN). Among these coumarin analogues, compounds 14, 16 and 18 were found to be potent molecules against HIV-1 IN at IC50 values of 0.96, 0.58, and 0.49 μM, respectively. The results provided a tool for guiding the further design of more potent antiviral agents and for predicting the affinity of related compounds. © 2007 Pharmaceutical Society of Japan.