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

[ Vol. 9 , Issue. 1 ]

Author(s):

Liying Zhang, Jizhe Dong, Jun Liu, Luyong Zhang, Lingyi Kong, Hequan Yao and Hongbin Sun   Pages 118 - 125 ( 8 )

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 PPAR γ agonistic activity and activated the transcription activity of PPAR γ 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.

Keywords:

Diabetes, Glycogen phosphorylase inhibitors, Oleanolic acid, PPAR γ agonists, Pentacyclic triterpene, Ursolic acid

Affiliation:

Jiangsu Center for Drug Screening, China Pharmaceutical University, Nanjing 21009, People’s Republic of China; and Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, Nanjing 21009, People’s Republic of China



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