title: Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing, Jiangsu 210009, China.
authors.forename: Peiqing
authors.initials: P
authors.lastname: Zhu
authors.forename: Yi
authors.initials: Y
authors.lastname: Bi
authors.forename: Jinyi
authors.initials: J
authors.lastname: Xu
authors.forename: Zan
authors.initials: Z
authors.lastname: Li
authors.forename: Jun
authors.initials: J
authors.lastname: Liu
authors.forename: Luyong
authors.initials: L
authors.lastname: Zhang
authors.forename: Wencai
authors.initials: W
authors.lastname: Ye
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Wu
mesh_terms: 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
chemical_list: C468651:23-hydroxybetulinic acid; D004791:Enzyme Inhibitors; D014315:Triterpenes; D024981:Glycogen Phosphorylase