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Elsevier, Bioorganic and Medicinal Chemistry Letters, 15(20), p. 4364-4366, 2010

DOI: 10.1016/j.bmcl.2010.06.070

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Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif

Journal article published in 2010 by Nina Klee, Pui Ee Wong, Beatriz Baragaña ORCID, Farah El Mazouni, Farah El Mazouni, Margaret A. Phillips, Michael P. Barrett, Ian H. Gilbert
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This paper is available in a repository.

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Abstract

Trypanosoma brucei, the parasite that causes human African trypanosomiasis, is auxotrophic for purines and has specialist nucleoside transporters to import these metabolites. In particular, the P2 aminopurine transporter can also selectively accumulate melamine derivatives. In this Letter, we report the coupling of the melamine moiety to 2-hydroxy APA, a potent ornithine decarboxylase inhibitor, with the aim of selectively delivering this compound to the parasite. The best compound described here shows an increased in vitro trypanocidal activity compared with the parent. (C) 2010 Elsevier Ltd. All rights reserved.