Inhibitory Effects of Triterpene–Azidothymidine Conjugates on Proliferation of Human Immunodeficiency Virus Type 1 and Its Protease

Abstract

The conjugates of some dicarboxylic acid hemiesters of triterpenes which show potent inhibition against human immunodeficiency virus type 1 protease (HIV-1 PR) with a reverse transcriptase inhibitor azidothymidine (AZT) or anti-HIV alkaloid FK 3000 were prepared, and their inhibitory activities were investigated against HIV-induced cytopathic effects (CPE) and HIV-1 PR. Most of the triterpene-AZT conjugates showed potent anti-HIV activity as well as moderate to potent PR inhibitory activity, though AZT itself showed no PR inhibitory activity at all. However, the triterpene-FK 3000 conjugates showed neither PR inhibitory activity nor anti-HIV activity.