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

被引：19
|
作者：
Chen, Zeng-Hao [1 ]
Wang, Ruo-Wen [1 ]
Qing, Feng-Ling [1 ,2 ]
机构：
[1] Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, Shanghai 200032, Peoples R China
[2] Donghua Univ, Coll Chem Chem Engn & Biotechnol, Shanghai 201620, Peoples R China
来源：
TETRAHEDRON LETTERS | 2012年 / 53卷 / 17期
基金：
中国国家自然科学基金;
关键词：
Dapagliflozin; SGLT2; inhibitor; Difluoromethylene; Diabetes; GLUCOSE; DISCOVERY; POTENT; ROUTE;
D O I：
10.1016/j.tetlet.2012.02.062
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
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. (c) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2171 / 2176
页数：6
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