Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Basic Information
ID: ALA4715716
Journal: Bioorg Med Chem Lett
Title: Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Authors: Ogawa AK,Bunte EV,Mal R,Lan P,Sun Z,Crespo A,Wiltsie J,Clemas J,Gibson J,Contino L,Lisnock J,Zhou G,Garcia-Calvo M,Jochnowitz N,Ma X,Pan Y,Brown P,Zamlynny B,Bateman T,Leung D,Xu L,Tong X,Liu K,Crook M,Sinclair P
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.
CiteXplore: 27161805
DOI: 10.1016/j.bmcl.2016.04.052
Patent ID: ┄