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 |
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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 > School of Infection & Immunity |
Journal Name: | Bioorganic and Medicinal Chemistry Letters |
ISSN: | 0960-894X |
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