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

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

Affiliation

  • 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.

Figures
Products