title: Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.
abstract: Prolylprolylisoxazoles and prolylprolylisoxazolines were synthesized through a 1,3-dipolar cycloaddition reaction. These compounds are potent inhibitors of human and trypanosomal prolyloligopeptidase. They were shown to inhibit Trypanosoma cruzi and Trypanosoma b. brucei in in vitro systems with ED(50)'s in the lower microM range.
authors: Department of Medicinal Chemistry, University of Antwerp, Belgium.
authors: Gunther
authors: G
authors: Bal
authors: Pieter
authors: P
authors: Van der Veken
authors: Dimitri
authors: D
authors: Antonov
authors: Anne-Marie
authors: AM
authors: Lambeir
authors: Philippe
authors: P
authors: Grellier
authors: Simon L
authors: SL
authors: Croft
authors: Koen
authors: K
authors: Augustyns
authors: Achiel
authors: A
authors: Haemers
mesh_terms: D000818:Animals; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D000085822:Prolyl Oligopeptidases; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D012697:Serine Endopeptidases / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects / Q000201:enzymology; D014351:Trypanosomatina / Q000187:drug effects
chemical_list: D007555:Isoxazoles; D011480:Protease Inhibitors; D014344:Trypanocidal Agents; D012697:Serine Endopeptidases; C000705287:PREPL protein, human; D000085822:Prolyl Oligopeptidases