Journal of Antibiotics p. 900 - 908 (1996)
Update date:2022-08-02
Topics:
Tsuda, Makoto
Muraoka, Yasuhiko
Someno, Tetsuya
Nagai, Machiko
Aoyagi, Takaaki
Takeuchi, Tomio
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.
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