2. Academic Validation
  3. 4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures

4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures

  • Bioorg Med Chem Lett. 2017 May 1;27(9):1902-1906. doi: 10.1016/j.bmcl.2017.03.034.
Masaki Meguro 1,  Satoru Miyauchi 2,  Yukiko Kanao 2,  Satoru Naito 2,  Kanae Suzuki 2,  Shinichi Inoue 2,  Keisuke Yamada 2,  Tsuyoshi Homma 2,  Kiyoshi Chiba 2,  Futoshi Nara 2,  Shinji Furuzono 2
Affiliations

Affiliations

  • 1 Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan. Electronic address: meguro.masaki.i2@daiichisankyo.co.jp.
  • 2 Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
PMID: 28359792 DOI: 10.1016/j.bmcl.2017.03.034
Abstract

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

Keywords

Aldosterone; Aldosterone synthase inhibitor; Amino-pyrimidine; CYP11B1; CYP11B2.

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