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学科主题: 氟化学
题名: Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs
其他题名: SGLT2抑制剂的合成和生物评价: gem-二氟亚甲基Dapagliflozin类似物
作者: Chen ZH(陈增浩) ; Wang RW(王若文) ; Qing FL(卿凤翎)
通讯作者: 卿凤翎
刊名: Tetrahedron Lett.
发表日期: 2012
卷: 53, 期:17, 页:2171-2176
收录类别: SCI
部门归属: 中科院上海有机化学研究所; 东华大学
英文摘要: 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.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000302587800007
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/28249
Appears in Collections:中科院有机氟化学重点实验室_期刊论文

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Recommended Citation:
Chen ZH,Wang RW,Qing FL. Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs[J]. Tetrahedron Lett.,2012,53(17):2171-2176.
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