Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase

被引:102
|
作者
Chen, J
Liu, J
Zhang, LY
Wu, GZ
Hua, WY
Wu, XM
Sun, HB
机构
[1] China Pharmaceut Univ, Coll Pharm, Ctr Drug Discovery, Nanjing 210009, Peoples R China
[2] China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Peoples R China
[3] China Pharmaceut Univ, Coll Pharm, Dept Pharmacol, Nanjing 210009, Peoples R China
关键词
oleanolic acid; glycogen phosphorylase; inhibitor; derivatives; diabetes;
D O I
10.1016/j.bmcl.2006.03.009
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Oleanolic acid and its synthetic derivatives have been identified as novel inhibitors of glycogen phosphorylase. Within this series of compounds, 4 (IC50 = 3.3 mu M) is the most potent GPa inhibitor. Preliminary structure-activity relationships of the oleanolic acid derivatives are discussed. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2915 / 2919
页数:5
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