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LI Jing, JIN Xiaoting, ZHANG Liying. Synthesis and biological evaluation of novel amide derivatives of pentacyclic triterterpenes as inhibitors of glycogen phosphorylase[J]. Journal of China Pharmaceutical University, 2016, 47(4): 422-428. DOI: 10.11665/j.issn.1000-5048.20160406
Citation: LI Jing, JIN Xiaoting, ZHANG Liying. Synthesis and biological evaluation of novel amide derivatives of pentacyclic triterterpenes as inhibitors of glycogen phosphorylase[J]. Journal of China Pharmaceutical University, 2016, 47(4): 422-428. DOI: 10.11665/j.issn.1000-5048.20160406

Synthesis and biological evaluation of novel amide derivatives of pentacyclic triterterpenes as inhibitors of glycogen phosphorylase

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  • 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.
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