title: Pentacyclic triterpenes. Part 5: synthesis and SAR study of corosolic acid derivatives as inhibitors of glycogen phosphorylases.
abstract: The synthesis and biological evaluation of corosolic acid derivatives and related compounds as inhibitors of rabbit muscle glycogen phosphorylase a is described. Within this series of compounds, 8 (IC(50)=7.31 microM), 12d (IC(50)=3.26 microM), and 12e (IC(50)=5.1 microM) exhibited more potent activities than the parent compound 1 (IC(50)=20 microM). SAR of these compounds is also discussed.
authors.affiliation: Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China.
authors.forename: Xiaoan
authors.initials: X
authors.lastname: Wen
authors.forename: Jun
authors.initials: J
authors.lastname: Xia
authors.forename: Keguang
authors.initials: K
authors.lastname: Cheng
authors.forename: Liying
authors.initials: L
authors.lastname: Zhang
authors.forename: Pu
authors.initials: P
authors.lastname: Zhang
authors.forename: Jun
authors.initials: J
authors.lastname: Liu
authors.forename: Luyong
authors.initials: L
authors.lastname: Zhang
authors.forename: Peizhou
authors.initials: P
authors.lastname: Ni
authors.forename: Hongbin
authors.initials: H
authors.lastname: Sun
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors*; D011817:Rabbits; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D014315:Triterpenes; C113861:corosolic acid; D024981:Glycogen Phosphorylase