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Synthesis of glucoconjugates of oleanolic acid as inhibitors of glycogen phosphorylase |
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| Authors: | Keguang Cheng Jun Liu Honglin Li Hongbin Sun Juan Xie |
| Affiliation: | a PPSM, ENS Cachan, CNRS, UniverSud, 61 av President Wilson, F-94230 CACHAN, France b Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China c Jiangsu Center for Drug Screening, China Pharmaceutical University, 1 Shennonglu, Nanjing 210038, China d Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China e School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China |
| Abstract: | Synthesis and biological evaluation of glucoconjugates of oleanolic acid, linked by either a triazole moiety or an ester function, as novel inhibitors of glycogen phosphorylase have been described. Several triterpene-glycoside conjugates exhibited moderate-to-good inhibitory activity against rabbit muscle GPa. Compound 12 showed the best inhibition with an IC50 value of 1.14 μM. Structure-activity relationship (SAR) analysis of these inhibitors is also discussed. Possible binding modes of compound 12 were explored by molecular docking simulations. |
| Keywords: | Glycogen phosphorylase Oleanolic acid Glucoconjugate Inhibitor Diabetes Click chemistry |
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