Study on betulin and betulinic acid derivatives aimed at developing anti-HIV agents effective against resistant virus

点击翻译按钮获取中文摘要

Based on our finding of a first-in-class drug candidate as a viral maturation inhibitor, bevirimat [3-O-(3',3'-dimethylsuccinyl)-betulinic acid], and potent anti-HIV active 3-O-acyl-(dihidro)betulin derivatives (e.g. 3-O-glutarydihydrobetulin and 3,28-di-O-dimethylsuccinylbetulin), a series of conjugates of 3,28-di-O-acylbetulin derivatives and HIV-reverse transcriptase inhibitor, AZT, as well as conjugates of 28-leucinyl-bevirimat and acyl-betulin derivatives were prepared and evaluated their anti-HIV activity. Several derivatives showed more potent anti-HIV activity than bevirimat.