Synthesis and Angiotensin Converting Enzyme-Inhibitory Activity of N-[(1S)-1-Carboxy-5-(4-piperidyl)pentyl]-L-alanine Derivatives

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概要

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• As part of a search for potent and long-lasting angiotensin converting enzyme (ACE) inhibitors, various types of N-[(1S)-1-carboxy-5-(4-piperidyl)pentyl]-L-alanine derivatives (7a, 8-11) were prepared. The key synthetic intermediate, N-[(1S)-5-(1-benzyloxycarbonyl-4-piperidyl)-1-ethoxycarbonylpentyl]-L-alanine (17a), was synthesized by asymmetric reduction of the α-oxoester (13) with Lactobacillus paracasei subsp. paracasei followed by a substitution reaction with tert-butyl L-alaninate (15) and subsequent treatment with hydrogen chloride. Compounds 7a and 8-11 showed potent and long-lasting ACE-inhibitory activity in rats.

• 社団法人日本薬学会の論文
• 1994-03-15

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

• 西川 浩平

  Pharmaceutical Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Industries

• 杉原 弘貞

  Pharmaceutical Research Laboratories I, 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.,

• 稲田 義行

  Pharmaceutical Research Laboratories, Takeda Chemical Industries, Ltd.,

• 加藤 武司

  Production Research Laboratories, Takeda Chemical Industries, Ltd.,

• 隅野 靖弘

  Technology Development Laboratories, 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.

• 加藤 武司

  Production Research Laboratories Takeda Chemical Industries Ltd.

• 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

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 隅野 靖弘

  Technology Development Laboratories Takeda Chemical Industries Ltd.

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