标题：Design, synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
作者：Zhao, Wen Jing; Shi, Yong Heng; Zhao, Gui Long; Wang, Yu Li; Shao, Hua; Tang, Li Da; Wang, Jian Wu
作者机构：[Zhao Wenjing] School of Chemistry and Chemical Engineering, Shandong University, Jinan, Shandong 250100, China.;[Wang Jianwu] School of Chemistry and 更多
通讯作者地址：[Zhao, GL]Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug Discovery, Tianjin 300193, Peoples R China.
关键词：Synthesis; C-Glucoside; SGLT2 inhibitor; Anti-hyperglycemic activity;; gem-Dimethyl
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. (C) 2011 Gui Long Zhao. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.