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.
Keywords: Eplerenone; Hypertension; Mineralocorticoid receptor antagonist; Spironolactone.
Copyright © 2016 Elsevier Ltd. All rights reserved.