期刊
TETRAHEDRON LETTERS
卷 53, 期 17, 页码 2171-2176出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2012.02.062
关键词
Dapagliflozin; SGLT2 inhibitor; Difluoromethylene; Diabetes
资金
- National Natural Science Foundation of China [21072028, 20832008]
- National Basic Research Program of China [2012CB21600]
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. (c) 2012 Elsevier Ltd. All rights reserved.
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