Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif |
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| Authors: | Nina Klee Pui Ee Wong Beatriz Baragaña Farah El Mazouni Margaret A. Phillips Michael P. Barrett Ian H. Gilbert |
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| Affiliation: | 1. Division of Biological Chemistry and Drug Discovery, College of Life Science, University of Dundee, Sir James Black Centre, Dundee DD1 5EH, UK;2. Division of Infection and Immunity and Wellcome Trust Centre for Molecular Parasitology, Glasgow Biomedical Research Centre, University of Glasgow G12 8TA, UK;3. UT Southwestern Medical Center at Dallas 6001 Forest Park, Dallas, TX 75390-9041, USA |
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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. |
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