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

被引：8

作者：

Meguro, Masaki ^{[1
]}

Miyauchi, Satoru ^{[1
]}

Kanao, Yukiko ^{[1
]}

Naito, Satoru ^{[1
]}

Suzuki, Kanae ^{[1
]}

Inoue, Shinichi ^{[1
]}

Yamada, Keisuke ^{[1
]}

Homma, Tsuyoshi ^{[1
]}

Chiba, Kiyoshi ^{[1
]}

Nara, Futoshi ^{[1
]}

Furuzono, Shinji ^{[1
]}

机构：

[1] Daiichi Sankyo Co Ltd, Shinagawa R&D Ctr, Shinagawa Ku, 1-2-58 Hiromachi, Tokyo 1408110, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 09期

关键词：

Aldosterone; CYP11B2; CYP11B1; Aldosterone synthase inhibitor; Amino-pyrimidine; IN-VIVO ACTIVITY; RHESUS-MONKEYS; HEART-FAILURE; DISCOVERY; POTENT; HYPERTENSION; DISEASE; LCI699; MICE;

D O I：

10.1016/j.bmcl.2017.03.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：1902 / 1906

页数：5

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