Article
Author: Inoue, Shinichi ; Meguro, Masaki ; Furuzono, Shinji ; Yamada, Keisuke ; Suzuki, Kanae ; Kanao-Arisumi, Yukiko ; Nara, Futoshi ; Naito, Satoru ; Miyauchi, Satoru ; Chiba, Kiyoshi ; Homma, Tsuyoshi
4-[(5-[2-Methyl-5-(methylsulfonyl)pentan-2-yl]sulfonylpyrimidin-4-yl)amino]benzonitrile 2 was identified as a novel potent aldosterone synthase inhibitor. Compound 2 was found to inhibit human CYP11B2 in the nanomolar range, and showed an aldosterone-lowering effect in a furosemide-treated cynomolgus monkey model. Although human CYP11B2 has the high homology sequence with human CYP11B1, compound 2 showed more than 80 times higher selectivity over human CYP11B1 in vitro.