标题:Design, Synthesis and Biological Activity of Tetrazole-bearing Uric Acid Transporter 1 Inhibitors
作者:Cai Wenqing; Liu Wei; Xie Yafei; Wu Jingwei; Liu Yuqiang; Liu Changying; Xu Weiren; Tang Lida; Wang Jianwu; Zhao Guilong
作者机构:[Cai Wenqing] School of Chemistry and Chemical Engineering, Shandong University, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Jinan, 更多
通讯作者:Wang, J(jwwang@sdu.edu.cn)
通讯作者地址:[Wang, JW]Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China;[Zhao, GL]Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug 更多
来源:高等学校化学研究
出版年:2017
卷:33
期:1
页码:49-60
DOI:10.1007/s40242-017-6351-3
关键词:URAT1 inhibitor; Structure-activity relationship; Drug discovery;; Lesinurad; Tetrazole; Bioisostere
摘要:Systematic structure-activity relationship(SAR) exploration of a moderately active tetrazole-bearing lesinurad-based hit if led to the discovery of a potent uric acid transporter 1(URAT1) inhibitor 1i, which possessed a novel molecular skeleton and was 11-fold more potent than the parent lesinurad against human URAT1 in-vitro (IC50=0.66 mu mol/L for ii vs. 7.18 mu mol/L for lesinurad).
收录类别:CSCD;SCOPUS;SCIE
WOS核心被引频次:5
Scopus被引频次:5
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-85009792086&doi=10.1007%2fs40242-017-6351-3&partnerID=40&md5=cd3a3c821fbafb2a56e6d1f8d3b5aaec
TOP