Synthesis and biological evaluation of novel amide derivatives of pentacyclic triterterpenes as inhibitors of glycogen phosphorylase
10.11665/j.issn.1000-5048.20160406
- VernacularTitle:五环三萜含氮衍生物的合成及糖原磷酸化酶抑制活性
- Author:
Jing LI
1
;
Xiaoting JIN
;
Liying ZHANG
Author Information
1. 承德医学院中药研究所，河北省中药研究与开发重点实验室
- Publication Type:Journal Article
- Keywords:
pentacyclic triterterpenes;
corosolic acid;
oleanolic acid;
glycogen phosphorylase inhibitor;
synthesis
- From:
Journal of China Pharmaceutical University
2016;47(4):422-428
- CountryChina
- Language:Chinese
-
Abstract:
Eight novel amide derivatives of corosolic acid were synthesized by acylation, amidation and hydrolysis reactions, etc. Six novel amide derivatives of oleanolic acid were synthesized by acylation, alkylation and reduction reactions, etc. Biological evaluation of the target compounds as inhibitors of glycogen phosphorylase(GP)has been described. Results indicated that eleven derivatives exhibited moderate-to-good inhibitory activities against glycogen phosphorylase. Among them, four target compounds possess better inhibition effects than lead compounds and compound 6 show the best inhibition effect with the IC50 of 11. 2 μmol/L.
