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	Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors
	Lv, Binhua1,2,3; Xu, Baihua1,2,3; Feng, Yan3; Peng, Kun3; Xu, Ge3; Du, Jiyan3; Zhang, Lili3; Zhang, Wenbin3; Zhang, Ting3; Zhu, Liangcheng3
刊名	Bioorganic & medicinal chemistry letters
	2009-12-15
卷号	19期号:24页码:6877-6881
关键词	O-spiroketal c-arylglucosides Sglt2 Spiro[isobenzofuran-1, 2 '-pyran] Glucosuria Blood glucose
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2009.10.088
通讯作者	Lv, binhua(51popo51@163.com)
英文摘要	A series of novel o-spiroketal c-arylglucosides have been prepared and evaluated in cell-based functional assays for activity against human sodium-dependent glucose co-transporters 1 and 2 ( sglt1 and 2). the core spiro[isobenzofuran-1,2'-pyran] structure proved to be an effective scaffold for diversification and a number of compounds with single digit nanomolar potency and high selectivity have been synthesized. compound 5a promoted glucosuria when administered in vivo in rats and produced a significant blood glucose reduction effect. (c) 2009 elsevier ltd. all rights reserved.
WOS关键词	REABSORPTION ; MUTATION ; TYPE-2 ; LEVEL
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
WOS类目	Chemistry, Medicinal ; Chemistry, Organic
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000271724200011
内容类型	期刊论文
URI标识	http://www.corc.org.cn/handle/1471x/2395065
专题	中国科学院大学
通讯作者	Lv, Binhua
作者单位	1.Chinese Acad Sci, Chengdu Inst Organ Chem, Chengdu 610041, Peoples R China 2.Chinese Acad Sci, Grad Sch, Beijing 100049, Peoples R China 3.Egret Pharma Shanghai Co Ltd, Shanghai 201203, Peoples R China 4.Theracos Inc, Sunnyvale, CA 94805 USA
推荐引用方式 GB/T 7714	Lv, Binhua,Xu, Baihua,Feng, Yan,et al. Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors[J]. Bioorganic & medicinal chemistry letters,2009,19(24):6877-6881.
APA	Lv, Binhua.,Xu, Baihua.,Feng, Yan.,Peng, Kun.,Xu, Ge.,...&Chen, Yuanwei.(2009).Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors.Bioorganic & medicinal chemistry letters,19(24),6877-6881.
MLA	Lv, Binhua,et al."Exploration of o-spiroketal c-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (sglt2) inhibitors".Bioorganic & medicinal chemistry letters 19.24(2009):6877-6881.

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