Title of article
Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs
Author/Authors
Chen، نويسنده , , Zeng-Hao and Wang، نويسنده , , Ruo-Wen and Qing، نويسنده , , Feng-Ling، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2012
Pages
6
From page
2171
To page
2176
Abstract
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.
Keywords
Dapagliflozin , SGLT2 inhibitor , Difluoromethylene , diabetes
Journal title
Tetrahedron Letters
Serial Year
2012
Journal title
Tetrahedron Letters
Record number
1880588
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