醛固酮合酶
化学
甾体11β-羟化酶
醛固酮
体外
盐皮质激素
酶抑制剂
速尿
化学合成
苯甲腈
ATP合酶
立体化学
酶
药理学
生物化学
肾素-血管紧张素系统
类固醇
内分泌学
受体
药物化学
生物
有机化学
激素
血压
作者
Masaki Meguro,Satoru Miyauchi,Yukiko Kanao-Arisumi,Satoru Naito,Kanae Suzuki,Shin‐ichi Inoue,Keisuke Yamada,Tsuyoshi Homma,Kiyoshi Chiba,Futoshi Nara,Shinji Furuzono
标识
DOI:10.1016/j.bmc.2024.117775
摘要
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.
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