Poststatin, a New Inhibitor of Prolyl Endopeptidase. VI. Endopeptidase Inhibitory Activity of Poststatin Analogues Containing Pyrrolidine Ring.
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- TSUDA MAKOTO
- Institute of Microbial Chemistry
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- MURAOKA YASUHIKO
- Institute of Microbial Chemistry
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- SOMENO TETSUYA
- Research and Development Division, Pharmaceuticals Group, Nippon Kayaku Co., Ltd.
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- NAGAI MACHIKO
- Institute of Microbial Chemistry
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- AoYAGI TAKAAKI
- Department of Hygienic Chemistry, Showa College of Pharmaceutical Sciences
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- TAKEUCHI TOMIO
- Institute of Microbial Chemistry
書誌事項
- タイトル別名
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- VI. Endopeptidase Inhibitory Activity of Poststatin Analogues Containing Pyrrolidine Ring
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説明
Several pyrrolidine-containing analogues of poststatin were synthesized and examined for their inhibitory activity against prolyl endopeptidase and cathepsin B in vitro. Replacement of the postine residue with 2-oxo-2-(2-pyrrolidinyl)acetic acid increased the selectivity and inhibitory activity against prolyl endopeptidase. Benzyloxycarbonyl-L-phenylalanyl-(S)-2-oxo-2-(2-pyrrolidinyl)acetyl-D-phenylalanine was about 46 times as active to prolyl endopeptidase as natural poststatin.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 49 (9), 900-908, 1996
公益財団法人 日本感染症医薬品協会