Pentacyclic triterpenes. Part 2: Synthesis and biological evaluation of maslinic acid derivatives as glycogen phosphorylase inhibitors

Xiaoan Wen; Pu Zhang; Jun Liu; Luyong Zhang; Xiaoming Wu; Peizhou Ni; Hongbin Sun

doi:10.1016/j.bmcl.2005.10.014

Pentacyclic triterpenes. Part 2: Synthesis and biological evaluation of maslinic acid derivatives as glycogen phosphorylase inhibitors

Bioorg Med Chem Lett. 2006 Feb;16(3):722-6. doi: 10.1016/j.bmcl.2005.10.014. Epub 2005 Oct 21.

Authors

Xiaoan Wen¹, Pu Zhang, Jun Liu, Luyong Zhang, Xiaoming Wu, Peizhou Ni, Hongbin Sun

Affiliation

¹ Department of Medicinal Chemistry, College of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.

PMID: 16246555
DOI: 10.1016/j.bmcl.2005.10.014

Abstract

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.

Publication types

Evaluation Study
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Glycogen Phosphorylase, Muscle Form / antagonists & inhibitors*
Muscles / enzymology
Rabbits
Structure-Activity Relationship
Triterpenes / chemical synthesis*
Triterpenes / pharmacology

Substances

Enzyme Inhibitors
Triterpenes
maslinic acid
Glycogen Phosphorylase, Muscle Form