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

Meguro, Masaki; Miyauchi, Satoru; Kanao, Yukiko; Naito, Satoru; Suzuki, Kanae; Inoue, Shinichi; Yamada, Keisuke; Homma, Tsuyoshi; Chiba, Kiyoshi; Nara, Futoshi; Furuzono, Shinji

Meguro, Masaki; Miyauchi, Satoru; Kanao, Yukiko; Naito, Satoru; Suzuki, Kanae; Inoue, Shinichi; Yamada, Keisuke; Homma, Tsuyoshi; Chiba, Kiyoshi; Nara, Futoshi; Furuzono, Shinji.

Afiliação

Meguro M; 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.
Miyauchi S; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Kanao Y; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Naito S; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Suzuki K; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Inoue S; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Yamada K; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Homma T; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Chiba K; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Nara F; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.
Furuzono S; Shinagawa R&D Center, Daiichi-Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8110, Japan.

Bioorg Med Chem Lett ; 27(9): 1902-1906, 2017 05 01.

Article em En | MEDLINE | ID: mdl-28359792

ABSTRACT

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.

Assuntos

Compostos de Anilina/química; Compostos de Anilina/farmacologia; Citocromo P-450 CYP11B2/antagonistas & inibidores; Inibidores Enzimáticos/química; Inibidores Enzimáticos/farmacologia; Pirimidinas/química; Pirimidinas/farmacologia; Citocromo P-450 CYP11B2/metabolismo; Células HEK293; Humanos

Palavras-chave

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

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Citocromo P-450 CYP11B2 / Inibidores Enzimáticos / Compostos de Anilina Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article

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