Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists. Issue 12 (15th June 2016)

• Record Type: Journal Article
• Authors: Ogawa, Anthony K.; Bunte, Ellen Vande; Mal, Rudrajit; Lan, Ping; Sun, Zhongxiang; Crespo, Alejandro; Wiltsie, Judyann; Clemas, Joseph; Gibson, Jack; Contino, Lisa; Lisnock, JeanMarie; Zhou, Gaochao; Garcia-Calvo, Margarita; Jochnowitz, Nina; Ma, Xiuying; Pan, Yi; Brown, Patricia; Zamlynny, Beata; Bateman, Thomas; Leung, Dennis; Xu, Ling; Tong, Xinchun; Liu, Kun; Crook, Martin; Sinclair, Peter
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 12(2016)
• Page Start: 2866
• Page End: 2869
• Publication Date: 2016-06-15
• Subjects: Mineralocorticoid receptor antagonist -- Hypertension -- Spironolactone -- Eplerenone; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.04.052
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Reported herein are a series of reverse indoles that represent novel non-steroidal mineralocorticoid receptor (MR) antagonists. The key structure–activity relationships (SAR) and acute pharmacodynamic efficacy in an acute natriuresis rodent model are presented. Abstract: 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.