Pentacyclic triterpenes. Part 2: Synthesis and biological evaluation of maslinic acid derivatives as glycogen phosphorylase inhibitors.
The synthesis of a series of maslinic acid derivatives is described and their effect on rabbit muscle glycogen phosphorylase a evaluated. Within this series of compounds, 15 (IC(50)=7 microM) is the most potent GPa inhibitor. SAR of the maslinic acid derivatives are discussed.
Wen
Xiaoan
X
Department of Medicinal Chemistry, College of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Zhang
Pu
P
Liu
Jun
J
Zhang
Luyong
L
Wu
Xiaoming
X
Ni
Peizhou
P
Sun
Hongbin
H
D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D024982:Glycogen Phosphorylase, Muscle Form / Q000037:antagonists & inhibitors*; D009132:Muscles / Q000201:enzymology; D011817:Rabbits; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D009828:Oleanolic Acid / Q000031:analogs & derivatives
D004791:Enzyme Inhibitors; D024982:Glycogen Phosphorylase, Muscle Form; D014315:Triterpenes; C412811:maslinic acid; D009828:Oleanolic Acid