Poststatin, a New Inhibitor of Prolyl Endopeptidase

VI. Endopeptidase Inhibitory Activity of Poststatin Analogues Containing Pyrrolidine Ring

抄録

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.