Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase.
Oleanolic acid and its synthetic derivatives have been identified as novel inhibitors of glycogen phosphorylase. Within this series of compounds, 4 (IC50 = 3.3 microM) is the most potent GPa inhibitor. Preliminary structure-activity relationships of the oleanolic acid derivatives are discussed.
Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Jun
J
Chen
Jun
J
Liu
Luyong
L
Zhang
Guanzhong
G
Wu
Weiyi
W
Hua
Xiaoming
X
Wu
Hongbin
H
Sun
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D003500:Cyclization; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D006943:Hyperglycemia / Q000097:blood; D051379:Mice; D015394:Molecular Structure; D009132:Muscles / Q000187:drug effects / Q000201:enzymology; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000737:chemistry; D011817:Rabbits; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D001786:Blood Glucose; D004791:Enzyme Inhibitors; D014315:Triterpenes; D009828:Oleanolic Acid; D024981:Glycogen Phosphorylase