Synthesis and Angiotensin converting Enzyme Inhibitory Activity of 1,5-Benzothiazepine and 1,5-Benzoxazepine Derivatives. II

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概要

• 論文の詳細を見る

• A series of (R)-3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-5-acetic acids (4 and 13)and (S)-3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetic acids (5 and 14) having an(S)-ω-amino-1-carboxyalkylamino group at the 3-position was prepared as part of our search for long-acting angiotensin converting enzyme (ACE) inhibitors. A number of derivatives had potent in vitro and in vivo ACE inhibitory activities. The structure-activity relationship of the series indicated that the duration of in vivo ACE inhibitory activity depends on the length of the carbon chain in the ω-aminoalkylamino substituent at the 3-position. The most prolonged activity was observed with (S)-8-amino-1-carboxyoctylamino derivatives (4d and 5d).

• 社団法人日本薬学会の論文
• 1986-05-25

著者

• 西川 浩平

  日本製薬株式会社研究本部

• 西川 浩平

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 伊藤 克己

  Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries

• 稲田 義行

  武田薬品工業株式会社研究推進部

• 郡 正城

  Pharmaceutical Research Laboratories, Takeda Chemical Industries, Ltd.,

• 郡 正城

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 稲田 義行

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 西川 浩平

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 川松 豊

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 杉原 弘貞

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 伊藤 克巳

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 伊藤 克巳

  武田薬品工業

• 伊藤 克已

  Central Research Division Takeda Chemical Industries Ltd.

• 川松 豊

  干寿製薬株式会社経営戦略室

• 郡 正城

  Pharmaceutical Research Laboratories Takeda Chemical Industries Ltd.

• 稲田 義行

  武田薬品工業株式会社 医療開拓研究本部

• 杉原 弘貞

  Central Research Division Takeda Chemical Industries. Ltd.

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