Synthesis And Pharmacological Activity Of Acylated Betulonic Acid Oxides And 28-Oxo-Allobetulone

摘要

In recent years, the chemical transformations and biological activity of triterpenoids of the lupane group have received much attention. It was found that betulin acylates possess antitumor properties [1], while lupeol esters with palmitic and linolic acids produce antiarrhythmic action [2]. The most promising inhibitors of HIV replication include 3-O-(3',3'-dimethylsuccinate) of betulinic acid and 3-O-(3',3'-dimethylsuccinate)-28-O-(2',2'-diniethylsuccmate) of betulin [3]. Recently, Kashiwada et al. [4] reported on the synthesis of derivatives of 3-alkylamino-3-deoxo-betulinic acid possessing anti-HIV-1 properties [4]. Another promising compound is betulin 3,28-di-O-nicotinate, which shows hepatoprotector, antiulcer, antiinflammatory, wound-healing, anti-HIV, and immunomodulant activity [5].