POSTSTATIN, A NEW INHIBITOR OF PROLYL ENDOPEPTIDASE .6. ENDOPEPTIDASEINHIBITORY ACTIVITY OF POSTSTATIN ANALOGS CONTAINING PYRROLIDINE RING

Several pyrrolidine-containing analogues of poststatin were synthesize d and examined for their inhibitory activity against prolyl endopeptid ase and cathepsin B in vitro. Replacement of the postine residue with 2-oxo-2-(2-pyrrolidinyl)acetic acid increased the selectivity and inhi bitory activity against prolyl endopeptidase. S)-2-oxo-2-(2-pyrrolidin yl)acetyl-D-phenyl-alanine alanine was about 46 times as active to pro lyl endopeptidase as natural poststatin.