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

Klee, N., Wong, P. E., Baragana, B., Mazouni, F. E., Phillips, M. A., Barrett, M.P. and Gilbert, I. H. (2010) Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif. Bioorganic and Medicinal Chemistry Letters, 20(15), pp. 4364-4366. (doi:10.1016/j.bmcl.2010.06.070)

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Publisher's URL: http://dx.doi.org/10.1016/j.bmcl.2010.06.070

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

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Barrett, Professor Michael
Authors: Klee, N., Wong, P. E., Baragana, B., Mazouni, F. E., Phillips, M. A., Barrett, M.P., and Gilbert, I. H.
College/School:College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
Journal Name:Bioorganic and Medicinal Chemistry Letters
ISSN:0960-894X

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