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Elsevier, Bioorganic and Medicinal Chemistry Letters, 17(13), p. 2875-2878, 2003

DOI: 10.1016/s0960-894x(03)00579-1

Wiley-VCH Verlag, ChemInform, 47(34), 2003

DOI: 10.1002/chin.200347185

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Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity

Journal article published in 2003 by Gunther Bal, van der Pieter Veken, Dimitri Antonov, Anne-Marie Lambeir ORCID, Philippe Grellier, Simon L. Croft, Koen Augustyns, Achiel Haemers
This paper is available in a repository.
This paper is available in a repository.

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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 ED(50)'s in the lower microM range.