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

被引：8
|
作者：
Zhang, Liying [2 ]
Dong, Jizhe [3 ]
Liu, Jun [1 ]
Zhang, Luyong [1 ]
Kong, Lingyi [4 ]
Yao, Hequan [4 ]
Sun, Hongbin [3 ,4 ]
机构：
[1] China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Jiangsu, Peoples R China
[2] Chengde Med Coll, Inst Tradit Chinese Med, Chengde 067000, Peoples R China
[3] China Pharmaceut Univ, Coll Pharm, Ctr Drug Discovery, Nanjing 21009, Jiangsu, Peoples R China
[4] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 21009, Jiangsu, Peoples R China
来源：
MEDICINAL CHEMISTRY | 2013年 / 9卷 / 01期
关键词：
Diabetes; Glycogen phosphorylase inhibitors; Oleanolic acid; PPAR gamma agonists; Pentacyclic triterpene; Ursolic acid; ACTIVATED-RECEPTOR-GAMMA; GLYCOGEN-PHOSPHORYLASE; INSULIN-RESISTANCE; INHIBITORS;
D O I：
10.2174/157340613804488413
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Synthesis and biological evaluation of a novel series of substituted pentacyclic triterpene derivatives as potential PPAR gamma agoinsts and glycogen phosphorylase inhibitors have been described. Compounds 11 and 17 showed potent PPAR gamma agonistic activity and activated the transcription activity of PPAR gamma 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.
引用
收藏
页码：118 / 125
页数：8
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