Synthesis and biological activity of heterocycle-fused derivatives of pentacylic triterpenes as glycogen phosphorylase inhibitors / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 491-496, 2009.
Article
in Chinese
| WPRIM
| ID: wpr-480361
ABSTRACT
Aim:
To search for novel modulators of glycogen metabolism through structural modifications of natural pentacyclic triterpenes.Methods:
A series of N-heterocyclic derivatives were synthesized by fusing indole, qui-noxaline and pyrazine rings with A-ring of oleanolic and ursolic acids. The compounds were biologically evaluated for their inhibitory activity against rabbit muscle glycogen phosphorylase. Results andConclusion:
Twelve heter-ocyclic triterpene derivatives were synthesized and their structures were confirmed by IR, ~1H NMR, ~(13)C NMR and MS. Except for compound 12, all of the compounds exhibited glycogen phosphorylase inhibitory activity with IC_(50) values in the range of 14-252 μmol/L Among this series of compounds, compound 15 showed the best potency with IC_(50), of 14 μmol/L
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of China Pharmaceutical University
Year:
2009
Type:
Article
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