Synthesis and biological evaluation of novel pentacyclic triterpene derivatives as potential PPARγ agonists.

Liying Zhang, Jizhe Dong, Jun Liu, Luyong Zhang, Lingyi Kong, Hequan Yao, Hongbin Sun

Institute of Traditional Chinese Medicine, Chengde Medical College, Chengde 067000, People’s Republic of China.

Medicinal chemistry (Shāriqah (United Arab Emirates)) 2013 Feb

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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.

Citation

Liying Zhang, Jizhe Dong, Jun Liu, Luyong Zhang, Lingyi Kong, Hequan Yao, Hongbin Sun. Synthesis and biological evaluation of novel pentacyclic triterpene derivatives as potential PPARγ agonists. Medicinal chemistry (Shāriqah (United Arab Emirates)). 2013 Feb;9(1):118-25