title: Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors.
abstract: New dicarboxylic acid bis(L-prolyl-pyrrolidine) amides were synthesized, and their inhibitory activity against prolyl oligopeptidase from pig brain was tested in vitro. As compared with earlier described prolyl oligopeptidase inhibitors, these new compounds have in common an L-prolyl-pyrrolidine moiety, but the typical lipophilic acyl end group is replaced by another L-prolyl-pyrrolidine moiety connected symmetrically with a short dicarboxylic acid linker. These compounds are a new type of peptidomimetic prolyl oligopeptidase inhibitor.
authors.affiliation: Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 1627, FIN-70211 Kuopio, Finland. wallen@uku.fi
authors.forename: Erik A A
authors.initials: EA
authors.lastname: Wallén
authors.forename: Johannes A M
authors.initials: JA
authors.lastname: Christiaans
authors.forename: Markus M
authors.initials: MM
authors.lastname: Forsberg
authors.forename: Jarkko I
authors.initials: JI
authors.lastname: Venäläinen
authors.forename: Pekka T
authors.initials: PT
authors.lastname: Männistö
authors.forename: Jukka
authors.initials: J
authors.lastname: Gynther
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D001921:Brain / Q000201:enzymology; D011392:Proline / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry; D000085822:Prolyl Oligopeptidases; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry; D012697:Serine Endopeptidases / Q000737:chemistry*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D000577:Amides; D011759:Pyrrolidines; D015842:Serine Proteinase Inhibitors; D011392:Proline; D012697:Serine Endopeptidases; D000085822:Prolyl Oligopeptidases