Design, Synthesis and Biological Activity of Tetrazole-bearing Uric Acid Transporter 1 Inhibitors

被引：10

作者：

Cai Wenqing ^{[1
,2
]}

Liu Wei ^{[2
]}

Xie Yafei ^{[2
]}

Wu Jingwei ^{[2
]}

Liu Yuqiang ^{[2
]}

Liu Changying ^{[2
]}

Xu Weiren ^{[2
]}

Tang Lida ^{[2
]}

Wang Jianwu ^{[1
]}

Zhao Guilong ^{[2
]}

机构：

[1] Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China

[2] Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug Discovery, Tianjin 300193, Peoples R China

来源：

CHEMICAL RESEARCH IN CHINESE UNIVERSITIES | 2017年 / 33卷 / 01期

关键词：

URAT1; inhibitor; Structure-activity relationship; Drug discovery; Lesinurad; Tetrazole; Bioisostere; GOUT; HYPERURICEMIA; DISEASE;

D O I：

10.1007/s40242-017-6351-3

中图分类号：

O6 [化学];

学科分类号：

070301 [无机化学];

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).

引用

收藏

页码：49 / 60

页数：12

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