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

Nina Klee, Pui Ee Wong, Beatriz Baragana, Farah El Mazouni, Margaret A. Phillips, Michael P. Barrett, Ian H. Gilbert

    Research output: Contribution to journalArticlepeer-review

    10 Citations (Scopus)
    9 Downloads (Pure)

    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.

    Original languageEnglish
    Pages (from-to)4364-4366
    Number of pages3
    JournalBioorganic & Medicinal Chemistry Letters
    Volume20
    Issue number15
    DOIs
    Publication statusPublished - 1 Aug 2010

    Keywords

    • Trypanosoma brucei
    • P2 transporter
    • Ornithine decarboxylase
    • UNUSUAL ADENOSINE TRANSPORTER
    • ORNITHINE-DECARBOXYLASE
    • CROSS-RESISTANCE
    • DIAMIDINE DRUGS
    • PENTAMIDINE
    • NITROHETEROCYCLES
    • POLYAMINES
    • FUTURE

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