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

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):5777-82. doi: 10.1016/j.bmcl.2007.08.057.
Xiaoan Wen  1 ,  Jun Xia ,  Keguang Cheng ,  Liying Zhang ,  Pu Zhang ,  Jun Liu ,  Luyong Zhang ,  Peizhou Ni ,  Hongbin Sun
Affiliations
  • 1. Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China.
PMID: 17869102 DOI: 10.1016/j.bmcl.2007.08.057
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.

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