Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists

被引：10

作者：

Ogawa, Anthony K. ^{[1
]}

Bunte, Ellen Vande ^{[1
]}

Mal, Rudrajit ^{[1
]}

Lan, Ping ^{[1
]}

Sun, Zhongxiang ^{[1
]}

Crespo, Alejandro ^{[2
]}

Wiltsie, Judyann ^{[1
]}

Clemas, Joseph ^{[1
]}

Gibson, Jack ^{[1
]}

Contino, Lisa ^{[1
]}

Lisnock, JeanMarie ^{[1
]}

Zhou, Gaochao ^{[1
]}

Garcia-Calvo, Margarita ^{[1
]}

Jochnowitz, Nina ^{[1
]}

Ma, Xiuying ^{[1
]}

Pan, Yi ^{[1
]}

Brown, Patricia ^{[1
]}

Zamlynny, Beata ^{[1
]}

Bateman, Thomas ^{[1
]}

Leung, Dennis ^{[2
]}

Xu, Ling ^{[2
]}

Tong, Xinchun ^{[2
]}

Liu, Kun ^{[1
]}

Crook, Martin ^{[1
]}

Sinclair, Peter ^{[1
]}

机构：

[1] Merck & Co Inc, Early Dev & Discovery Sci, 2000 Galloping Hill Rd, Kenilworth, NJ 07033 USA

[2] Merck & Co Inc, Early Dev & Discovery Sci, 126 E Lincoln Ave, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 12期

关键词：

Mineralocorticoid receptor antagonist; Hypertension; Spironolactone; Eplerenone; MILD PATIENTS HOSPITALIZATION; ALDOSTERONE; EPLERENONE; POTENT; IDENTIFICATION; HYPERKALEMIA; SURVIVAL;

D O I：

10.1016/j.bmcl.2016.04.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Reported herein are a series of reverse indoles that represent novel non-steroidal mineralocorticoid receptor (MR) antagonists. The key structure-activity relationships (SAR) are presented below. This reverse indole series is exemplified by a compound that demonstrated efficacy in an acute natriuresis rodent model comparable to marketed MR antagonists, spironolactone and eplerenone. (C) 2016 Elsevier Ltd. All rights reserved.

引用

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页码：2866 / 2869

页数：4

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