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Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites

Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites

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Authors

  • Alessandro Baliani
  • Valerie Peal
  • Ludovic Gros
  • Reto Brun
  • Marcel Kaiser
  • Michael P. Barrett
  • Ian H. Gilbert

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Original languageEnglish
Pages1154-1166
Number of pages13
JournalOrganic and Biomolecular Chemistry
Journal publication date2009
Volume7
Issue6
DOIs
StatePublished

Abstract

Human African trypanosomiasis (HAT), caused by the protozoan parasite Trypanosoma brucei spp., is a major health problem in sub-Saharan Africa. New drugs are urgently required for the disease. Selective uptake of toxic compounds into trypanosomes has been achieved by exploiting plasma membrane transporters. For example, the P2 aminopurine transporter, along with other transporters, selectively concentrates melamine and benzamidine moieties into trypanosomes. We have previously reported the use of the melamine motif to selectively target nitrofuran to the trypanosome. In this paper we report the further investigation of the structure activity relationships and the effect of the introduction of different functionalized substituents onto the melamine unit. Most of the compounds tested in vitro for their trypanocidal activity showed activities in the submicromolar range against T. b. rhodesiense.

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