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

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...

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Detalles Bibliográficos
Autores principales: Klee, Nina, Wong, Pui Ee, Baragaña, Beatriz, Mazouni, Farah El, Phillips, Margaret A., Barrett, Michael P., Gilbert, Ian H.
Formato: Texto
Lenguaje:English
Publicado: Elsevier Science Ltd 2010
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2935964/
https://www.ncbi.nlm.nih.gov/pubmed/20615694
http://dx.doi.org/10.1016/j.bmcl.2010.06.070
Descripción
Sumario: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.

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