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WEN Xiao-an, ZHANG Ying-xia, LIU Jun, ZHANG Lu-yong, NI Pei-zhou, SUN Hong-bin. Synthesis and biological activity of heterocycle-fused derivatives of pentacylic triterpenes as glycogen phosphorylase inhibitors[J]. Journal of China Pharmaceutical University, 2009, 40(6): 491-496.
Citation: WEN Xiao-an, ZHANG Ying-xia, LIU Jun, ZHANG Lu-yong, NI Pei-zhou, SUN Hong-bin. Synthesis and biological activity of heterocycle-fused derivatives of pentacylic triterpenes as glycogen phosphorylase inhibitors[J]. Journal of China Pharmaceutical University, 2009, 40(6): 491-496.
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Synthesis and biological activity of heterocycle-fused derivatives of pentacylic triterpenes as glycogen phosphorylase inhibitors

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  • 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，quinoxaline 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 and Conclusion ：Twelve heterocyclic triterpene derivatives were synthesized and their structures were confirmed by IR，1H NMR，13C NMR and MS.Except for compound 12 ，all of the compounds exhibited glycogen phosphorylase inhibitory activity with IC50 values in the range of 14-252 μmol/L.Among this series of compounds，compound 15 showed the best potency with IC50 of 14 μmol/L.
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