Pentacyclic triterpenes. Part 5: Synthesis and SAR study of corosolic acid derivatives as inhibitors of glycogen phosphorylases

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 (IC50 = 7.31 μM), 12d (IC50 = 3.26 μM), and 12e (IC50 = 5.1 μM) exhibited more potent activities than the parent compound 1 (IC50 = 20 μM). SAR of these compounds is also discussed.

The synthesis and biological evaluation of corosolic acid derivatives as inhibitors of glycogen phosphorylase is described.Figure optionsDownload as PowerPoint slide