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

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	Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs
	Chen ZH(陈增浩) ; Wang RW(王若文) ; Qing FL(卿凤翎)
刊名	Tetrahedron Lett.
	2012
卷号	53 期号:17 页码:2171-2176
ISSN号	0040-4039
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
通讯作者	卿凤翎
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.
学科主题	氟化学
收录类别	SCI
原文出处	http://dx.doi.org/10.1016/j.tetlet.2012.02.062
语种	英语
WOS记录号	WOS:000302587800007
公开日期	2013-08-23
内容类型	期刊论文
源URL	[http://202.127.28.38/handle/331003/28249]
专题	上海有机化学研究所_中科院有机氟化学重点实验室
推荐引用方式 GB/T 7714	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.
APA	陈增浩,王若文,&卿凤翎.(2012).Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs.Tetrahedron Lett.,53(17),2171-2176.
MLA	陈增浩,et al."Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin analogs".Tetrahedron Lett. 53.17(2012):2171-2176.