Poststatin, a new inhibitor of prolyl endopeptidase. VI. Endopeptidase inhibitory activity of poststatin analogues containing pyrrolidine ring.

…, Y Muraoka, T Someno, M Nagai, T AoYAGI…

文献索引：Tsuda, Makoto; Muraoka, Yasuhiko; Someno, Tetsuya; Nagai, Machiko; Aoyagi, Takaaki; Takeuchi, Tomio Journal of Antibiotics, 1996 , vol. 49, # 9 p. 900 - 908

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被引用次数: 9

摘要

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 ...