Synthesis and Biological Evaluation of Novel Pentacyclic Triterpene Derivatives as Potential PPARγ Agonists

Title:Synthesis and Biological Evaluation of Novel Pentacyclic Triterpene Derivatives as Potential PPARγ Agonists

Volume: 9 Issue: 1

Author(s): Liying Zhang, Jizhe Dong, Jun Liu, Luyong Zhang, Lingyi Kong, Hequan Yao and Hongbin Sun

Affiliation:

Keywords: Diabetes, Glycogen phosphorylase inhibitors, Oleanolic acid, PPARγ agonists, Pentacyclic triterpene, Ursolic acid

Abstract: Synthesis and biological evaluation of a novel series of substituted pentacyclic triterpene derivatives as potential PPARγ agoinsts and glycogen phosphorylase inhibitors have been described. Compounds 11 and 17 showed potent PPARγ agonistic activity and activated the transcription activity of PPARγ in a dose-dependent manner. On the other hand, eleven compounds exhibited moderate inhibitory activity against rabbit muscle glycogen phosphorylase a (RMGPa), and triterpene 10 was the best one. Structure-activity relationship (SAR) is also discussed.

Cite this article as:

Zhang Liying, Dong Jizhe, Liu Jun, Zhang Luyong, Kong Lingyi, Yao Hequan and Sun Hongbin, Synthesis and Biological Evaluation of Novel Pentacyclic Triterpene Derivatives as Potential PPARγ Agonists, Medicinal Chemistry 2013; 9 (1) . https://dx.doi.org/10.2174/1573406411309010118