Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.

Gunther Bal ; Pieter Van der Veken ; Dimitri Antonov ; Anne-Marie Lambeir ; Philippe Grellier ; Simon L Croft ORCID logo ; Koen Augustyns ; Achiel Haemers ; (2003) Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity. Bioorganic & medicinal chemistry letters, 13 (17). pp. 2875-2878. ISSN 0960-894X DOI: 10.1016/s0960-894x(03)00579-1
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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.
Item Type Article
Keywords Alpha-keto heterocycles, prolyl oligopeptidase, trypanosoma-, cruzi, in-vitro, endopeptidase, ring, isoxazolines, elastase, library, design
ISI 184865300012
Date Deposited 17 Oct 2011 21:32

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