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Design,synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors |
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| Authors: | Wen Jing Zhaoa Yong Heng Shi Gui Long Zhao Yu Li Wangb Hua Shaob Li Da Tangb Jian Wu Wang a School of Chemistry Chemical Engineering Sh ong University Jinan China b Tianjin Key Laboratory of Molecular Design Drug Discovery Tianjin Institute of Pharmaceutical Research Tianjin China c School of Pharmacy Tianjin Medical University Tianjin China |
| Institution: | a School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China;b Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;c School of Pharmacy, Tianjin Medical University, Tianjin 300070, China |
| Abstract: | A series of gem-dimethyl-bearing C-glucosides were designed and synthesized as SGLT2 inhibitors,with anhydrous aluminum chloride-mediated Friedel-Crafts alkylation to construct the gem-dimethyl functionality being the key step.The in vivo anti-hyperglycemic activity was evaluated with mice oral glucose tolerance test(OGTT),and all the synthesized compounds showed significant but less potent anti-hyperglycemic activity than the positive control dapagliflozin. |
| Keywords: | Synthesis C-Glucoside SGLT2 inhibitor Anti-hyperglycemic activity gem-Dimethyl |
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