Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase.
A series of 23-hydroxybetulinic acid derivatives were prepared and tested in vitro as a new class of inhibitors of glycogen phosphorylase (GP). Within this series of compounds, 12b (IC(50)=3.5 microM) is the most potent GPa inhibitor. The preliminary SAR results of the 23-hydroxybetulinic acid derivatives are discussed.
Zhu
Peiqing
P
Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing, Jiangsu 210009, China.
Bi
Yi
Y
Xu
Jinyi
J
Li
Zan
Z
Liu
Jun
J
Zhang
Luyong
L
Ye
Wencai
W
Wu
Xiaoming
X
D000818:Animals; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors*; D006801:Humans; D011817:Rabbits; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
C468651:23-hydroxybetulinic acid; D004791:Enzyme Inhibitors; D014315:Triterpenes; D024981:Glycogen Phosphorylase