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

共 50 条

[41] Synthesis,Crystal Structure and Neuroprotection of Methyl 2-((4-(2-(2-Methylphenoxy)acetyl)-piperazin-1-yl)-methyl)benzoate
仲琰
王垚
王晶
许逸
李萍
吴斌
结构化学, 2014, 33 (07) : 1096 - 1101
[42] Synthesis and antimicrobial activity of novel 2-[4-(1H-benzimidazol-1-yl)phenyl]-1H-benzimidazoles
Alp, Mehmet
Goker, Ali Hakan
Altanlar, Nurten
TURKISH JOURNAL OF CHEMISTRY, 2014, 38 (01) : 152 - 156
[43] 1-{2-( 4-Chlorobenzyloxy)-2-[4-(morpholin- 4- yl) phenyl] ethyl}-1H-benzimidazole propan-2-ol monosolvate
Guven, Ozden Ozel
Capanlar, Seval
Adler, Philip D. F.
Coles, Simon J.
Hokelek, Tuncer
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2013, 69 : O1437 - +
[44] 1-[1-(4-Chlorobenzenesulfonyl)-1H-indole-3-yl]-3-[4-(pyridin-2-yl)piperazin-1-yl]propan-1-one
Diethelm, Benjamin
Almendras, Sebastian
Recabarren-Gajardo, Gonzalo
MOLBANK, 2018, (02)
[45] 2-[4-(1H-1,2,4-Triazol-1-yl) phenyl]-1Hbenzimidazole
Cheng, Long-Huai
Zheng, Zheng
Han, Zhi-Li
Wu, Zhi-Chao
Zhou, Hong-Ping
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2012, 68 : O2890 - +
[46] Anxiolytic-like effect of 2-(4-((1-phenyl-1H-pyrazol-4-yl)methyl)piperazin-1-yl)ethan-1-ol is mediated through the benzodiazepine and nicotinic pathways
Brito, Adriane F.
Fajemiroye, James O.
Neri, Hiasmin F. S.
Silva, Dayane M.
Silva, Daiany P. B.
Sanz, German
Vaz, Boniek G.
de Carvalho, Flavio S.
Ghedini, Paulo C.
Liao, Luciano M.
Menegatti, Ricardo
Costa, Elson A.
CHEMICAL BIOLOGY & DRUG DESIGN, 2017, 90 (03) : 432 - 442
[47] Synthesis of Benzyl 2-(4-(8-chloro-5H-dibenzo[b,e][1,4] diazepin-11-yl)piperazin-1-yl) acetate
Camerino, Michelle A.
Capuano, Ben
Crosby, Ian T.
Lloyd, Edward J.
MOLBANK, 2005, (06)
[48] Crystal structure of 3-{[4-(2-methoxyphenyl)piperazin-1-yl] methyl}-5-(thiophen-2-yl)-1,3,4-oxadiazole-2(3H)-thione
Al-Alshaikh, Monirah A.
Abuelizz, Hatem A.
El-Emam, Ali A.
Abdelbaky, Mohammed S. M.
Garcia-Granda, Santiago
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2016, 72 : 269 - +
[49] Ethyl 2-[4-(dimethylamino) phenyl]-1-phenyl-1H-benzimidazole-5-carboxylate
Yeong, Keng Yoon
Ali, Mohamed Ashraf
Choon, Tan Soo
Rosli, Mohd Mustaqim
Razak, Ibrahim Abdul
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS, 2013, 69 : O886 - +
[50] N-{2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl}pyridin-2-amine monohydrate
Jiang, Quan-Fu
Lu, Chun-Xiong
ACTA CRYSTALLOGRAPHICA SECTION E-STRUCTURE REPORTS ONLINE, 2010, 66 : O1727 - U766

← 1 2 3 4 5 →