Design,synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors
Design,synthesis and in vivo anti-hyperglycemic activity of gem-dimethyl-bearing C-glucosides as SGLT2 inhibitors作者机构:School of Chemistry and Chemical Engineering Shandong University Jinan 250100 China Tianjin Key Laboratory of Molecular Design and Drug Discovery Tianjin Institute of Pharmaceutical Research Tianjin 300193 China School of Pharmacy Tianjin Medical University Tianjin 300070 China
出 版 物:《Chinese Chemical Letters》 (中国化学快报(英文版))
年 卷 期:2011年第22卷第10期
页 面:1215-1218页
核心收录:
学科分类:0832[工学-食品科学与工程(可授工学、农学学位)] 081702[工学-化学工艺] 08[工学] 0817[工学-化学工程与技术] 083203[工学-农产品加工及贮藏工程]
基 金:Key Projects of Tianjin Science and Technology Support Plan(No. 10ZCKFSH01300) for financial support
主 题: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 *** 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.