引用本文:
Wen Jing Zhao, Yong Heng Shi, Gui Long Zhao, Yu Li Wang, Hua Shao, Li Da Tang, Jian Wu Wang. Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors[J]. Chinese Chemical Letters,
2011, 22(10): 1215-1218.
doi:
10.1016/j.cclet.2011.05.022
Citation: Wen Jing Zhao, Yong Heng Shi, Gui Long Zhao, Yu Li Wang, Hua Shao, Li Da Tang, Jian Wu Wang. Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors[J]. Chinese Chemical Letters, 2011, 22(10): 1215-1218. doi: 10.1016/j.cclet.2011.05.022
Citation: Wen Jing Zhao, Yong Heng Shi, Gui Long Zhao, Yu Li Wang, Hua Shao, Li Da Tang, Jian Wu Wang. Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors[J]. Chinese Chemical Letters, 2011, 22(10): 1215-1218. doi: 10.1016/j.cclet.2011.05.022
Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
摘要:
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.
English
Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
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.
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Key words:
- Synthesis
- / C-Glucoside
- / SGLT2 inhibitor
- / Anti-hyperglycemic activity
- / gem-Dimethyl
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