Prolylisoxazoles: Potent inhibitors of prolyloligopeptidase with antitrypanosomal activity


Bal, G; van der Veken, P; Antonov, D; Lambeir, AM; Grellier, P; Croft, SL; Augustyns, K; Haemers, A; (2003) Prolylisoxazoles: Potent inhibitors of prolyloligopeptidase with antitrypanosomal activity. Bioorganic & medicinal chemistry letters, 13 (17). pp. 2875-2878. ISSN 0960-894X DOI: https://doi.org/10.1016/s0960-894x(03)00579-1

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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 ED50'S in the lower muM range. (C) 2003 Elsevier Ltd. All rights reserved.

Item Type: Article
Keywords: Alpha-keto heterocycles, prolyl oligopeptidase, trypanosoma-, cruzi, in-vitro, endopeptidase, ring, isoxazolines, elastase, library, design
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Research Centre: Malaria Centre
PubMed ID: 14611847
Web of Science ID: 184865300012
URI: http://researchonline.lshtm.ac.uk/id/eprint/15840

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