Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists

…, T Tanaka, N Habuka, S Sogabe, M Ono…

Index: Hasui, Tomoaki; Matsunaga, Nobuyuki; Ora, Taiichi; Ohyabu, Norio; Nishigaki, Nobuhiro; Imura, Yoshimi; Igata, Yumiko; Matsui, Hideki; Motoyaji, Takashi; Tanaka, Toshimasa; Habuka, Noriyuki; Sogabe, Satoshi; Ono, Midori; Siedem, Christopher S.; Tang, Tony P.; Gauthier, Cassandra; De Meese, Lisa A.; Boyd, Steven A.; Fukumoto, Shoji Journal of Medicinal Chemistry, 2011 , vol. 54, # 24 p. 8616 - 8631

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Citation Number: 34

Abstract

Mineralocorticoid receptor (MR) blockade has come into focus as a promising approach for the treatment of cardiovascular diseases such as hypertension and congestive heart failure. In order to identify a novel class of nonsteroidal MR antagonists that exhibit significant potency and good selectivity over other steroidal hormone receptors, we designed a novel series of benzoxazin-3-one derivatives and synthesized them from 6-(7 H-[1, 2, 4] triazolo [ ...