Article ID Journal Published Year Pages File Type
5273620 Tetrahedron Letters 2012 6 Pages PDF
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.

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Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry