4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures. Issue 9 (1st May 2017)

• Record Type: Journal Article
• Authors: Meguro, Masaki; Miyauchi, Satoru; Kanao, Yukiko; Naito, Satoru; Suzuki, Kanae; Inoue, Shinichi; Yamada, Keisuke; Homma, Tsuyoshi; Chiba, Kiyoshi; Nara, Futoshi; Furuzono, Shinji
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 9(2017)
• Page Start: 1902
• Page End: 1906
• Publication Date: 2017-05-01
• Subjects: Aldosterone -- CYP11B2 -- CYP11B1 -- Aldosterone synthase inhibitor -- Amino-pyrimidine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.03.034
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 2, 2, 2-Trifluoro-1-{4-[(4-fluorophenyl)amino]pyrimidin-5-yl}-1-[1-(methylsulfonyl)piperidin-4-yl]ethanol1 was identified as a novel potent aldosterone synthase inhibitor. Despite large species differences, compound1 inhibits both human and rodent CYP11B2 in a nano-molar range.