Synthesis of Prolyl Endopeptidase Inhibitors and Evaluation of Their Structure-Activity Relationships : In Vitro Inhibition of Prolyl Endopeptidase from Canine Brain

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概要

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• By chemical modification of a known prolyl endopeptidase (PEP) inhibitor (N-[N-(4-phenylbutanoyl)-L-prolyl]pyrrolidine; SUAM-1221), several arylalkanoyl derivatives (V-1-27) were synthesized and tested for in vitro inhibitory activity towards PEP from canine brain. Among them, 4-(2-thienyl)butanoyl derivatives (V-24-27) showed more potent PEP-inhibitory activity than SUAM-1221. The structure-activity relationships of these compounds are discussed.

• 社団法人日本薬学会の論文
• 1993-09-15

著者

• 小林 直美

  ゼリア新薬工業株式会社中央研究所薬理研究部

• 吉長 幸嗣

  ゼリア新薬工業 (株)

• 吉長 幸嗣

  ぜリア新薬工業(株)中央研究所

• 池田 勇五

  ゼリア新薬工業(株)中央研究所

• 新井 平八郎

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 西岡 裕康

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 丹羽 誠一

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 山中 健史

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 田中 芳明

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 吉長 幸嗣

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 小林 直美

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 三浦 直良

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 池田 勇五

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• 田中 芳明

  ゼリア新薬工業株式会社中央研究所薬理研究部

• 山中 健史

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• 丹羽 誠一

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• 新井 平八郎

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• 三浦 直良

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• 西岡 裕康

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

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