Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists

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. [Display omitted] 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.