Synthesis of Human Renin Inhibitory Peptides, Angiotensinogen Transition-State Analogs Containing a Retro-Inverso Amide Bond
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概要
- 論文の詳細を見る
The experimental details for the synthesis of human renin inhibitors are described. In order to aviod metabolic degradation of the Phe-His (P_3-P_2) amide bond in transition-state analogs, structurally modified acyl residues (P_4-P_3) were incorporated into the inhibitors. Compound 1a, which contained 2-(1-naphthylmethyl)-3-(N-phenethylcarbamoyl)propionyl residue (P_4-P_3) with a retro-inverso amide bond, L-histidine, and norstatine isoamylamide residue (P_1-P_1') as a transition-state mimic, had potent human renin inhibitory activity, and it lowered blood pressure when administered orally to common marmosets.
- 社団法人日本薬学会の論文
- 1990-11-25
著者
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赤羽 健司
キッセイ薬品工業株式会社中央研究所
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椿 敦
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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中野 泰志
キッセイ薬品工業株式会社中央研究所
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原田 弘
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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飯塚 欣二
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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上條 哲聖
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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赤羽 健司
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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山本 亮治
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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中野 泰志
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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久保田 哲弘
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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島岡 巌
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,
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梅山 秀明
School of Pharmaceutical Sciences, Kitasato University
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木曽 良明
Department of Medicinal Chemistry, Kyoto Pharmaceutical University
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上條 哲聖
キッセイ薬品工業株式会社中央研究所
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上条 哲聖
キッセイ薬品工業中央研究所
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久保田 哲弘
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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梅山 秀明
School Of Pharmaceutical Sciences Kitasato University
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山本 亮治
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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飯塚 欣二
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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木曽 良明
Department Of Medicinal Chemistry Kyoto Pharmaceutical University
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原田 弘
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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島岡 巌
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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赤羽 健司
Central Research Laboratories Kissei Pharmaceutical Co. Ltd.
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