Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs

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• 作者：Zeng-Hao Chen^a ; Ruo-Wen Wang^a ; Feng-Ling Qing^a ; ^b ; ^{flq@mail.sioc.ac.cn}
• 关键词：Dapagliflozin ; SGLT2 inhibitor ; Difluoromethylene ; Diabetes
• 刊名：Tetrahedron Letters
• 出版年：2012
• 期刊代码：109_00404039
• 类别：ch
• 出版时间：25 April, 2012
• 卷：53
• 期：17
• 页码：2171-2176
• 文件大小：1187 K

摘要

Dapagliflozin is currently the most advanced SGLT2 inhibitor, which has been used in Phase III clinical trials for treatment of diabetes. Here we describe the design and synthesis of Dapagliflozin analogs modified with gem-difluoromethylene group. Their biological evaluation of in vitro inhibitory activity against human SGLT2 showed that some of the analogs with CF₂ at C-4 are better SGLT2 inhibitors compared with Dapagliflozin.