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

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

Research output: Contribution to journalArticle

10 Scopus citations

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.

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

Keywords

  • Ornithine decarboxylase
  • P2 transporter
  • Trypanosoma brucei

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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