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. 2016 Jun 15;26(12):2866-2869.
doi: 10.1016/j.bmcl.2016.04.052. Epub 2016 Apr 20.

Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists

Anthony K Ogawa  1 , Ellen Vande Bunte  1 , Rudrajit Mal  1 , Ping Lan  1 , Zhongxiang Sun  1 , Alejandro Crespo  2 , Judyann Wiltsie  1 , Joseph Clemas  1 , Jack Gibson  1 , Lisa Contino  1 , JeanMarie Lisnock  1 , Gaochao Zhou  1 , Margarita Garcia-Calvo  1 , Nina Jochnowitz  1 , Xiuying Ma  1 , Yi Pan  1 , Patricia Brown  1 , Beata Zamlynny  1 , Thomas Bateman  1 , Dennis Leung  2 , Ling Xu  2 , Xinchun Tong  2 , Kun Liu  1 , Martin Crook  1 , Peter Sinclair  1
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Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists

Anthony K Ogawa et al. Bioorg Med Chem Lett. .

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.

Keywords: Eplerenone; Hypertension; Mineralocorticoid receptor antagonist; Spironolactone.

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