标题:3-Oxodapagliflozin as a Potent and Highly Selective SGLT2 Inhibitor for the Treatment of Type 2 Diabetes
作者:Zhang Shuo; Wang Yuli; Liu Wei; Xie Yafei; Liu Yuqiang; Xu Weiren; Tang Lida; Wang Jianwu; Zhao Guilong
作者机构:[Zhang, S] School of Chemistry and Chemical Engineering, Shandong University, Jinan, 250100, China, Tianjin Key Laboratory of Molecular Design and Dru 更多
通讯作者地址:[Wang, JW]Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China.
来源:高等学校化学研究(英文版)
出版年:2014
卷:30
期:5
页码:785-793
DOI:10.1007/s40242-014-4043-9
关键词:SGLT2 inhibitor;Structure-activity relationship;Dapagliflozin
摘要:Structural modifications of 3-OH in the glucose moiety of dapagliflozin(1), an approved potent sodium-dependent glucose transporter 2(SGLT2) inhibitor, led to 3-oxodapagliflozin(16), a highly potent and more selective SGLT2 inhibitor[IC50(hSGLT1)/IC50(hSGLT2)=2851 for compound 16 vs. 843 for compound 1]. 3-Oxodapagliflozin(16) exhibited in vitro(IC50=1.0 nmol/L against hSGLT2 for compound 16 vs. 1.3 nmol/L for compound 1) and in vivo activities comparable to those of dapagliflozin(1). The bioactivities of 3-oxodapagliflozin (16) warrant its further evaluation as a promising SGLT2 inhibitor for the treatment of type 2 diabetes.
收录类别:CSCD;SCOPUS;SCIE
Scopus被引频次:1
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84909636317&doi=10.1007%2fs40242-014-4043-9&partnerID=40&md5=e7c6dc506877c585919fd20f77ad7da6
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