Discovery of a novel sub-class of ROMK channel inhibitors typified by 5-(2-(4-(2-(4-(1H-Tetrazol-1-yl)phenyl)acetyl)piperazin-1-yl) ethyl)isobenzofuran-1(3H)-one

被引：24

作者：

Tang, Haifeng ^{[1
]}

de Jesus, Reynald K.

Walsh, Shawn P.

Zhu, Yuping

Yan, Yan

Priest, Birgit T.

Swensen, Andrew M.

Alonso-Galicia, Magdalena

Felix, John P.

Brochu, Richard M.

Bailey, Timothy

Thomas-Fowlkes, Brande

Zhou, Xiaoyan

Pai, Lee-Yuh

Hampton, Caryn

Hernandez, Melba

Owens, Karen

Roy, Sophie

Kaczorowski, Gregory J.

Yang, Lihu

Garcia, Maria L.

Pasternak, Alexander

机构：

[1] Dept Med Chem, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 21期

关键词：

ROMK; Hypertension; Heart failure; Diuresis; Natriuresis; POTASSIUM CHANNEL; BLOOD-PRESSURE; CLONING; KIR1.1;

D O I：

10.1016/j.bmcl.2013.08.104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A sub-class of distinct small molecule ROMK inhibitors were developed from the original lead 1. Medicinal chemistry endeavors led to novel ROMK inhibitors with good ROMK functional potency and improved hERG selectivity. Two of the described ROMK inhibitors were characterized for the first in vivo proof-of-concept biology studies, and results from an acute rat diuresis model confirmed the hypothesis that ROMK inhibitors represent new mechanism diuretic and natriuretic agents. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：5829 / 5832

页数：4

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