Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors

Gordon J. Florence (Lead / Corresponding author), Andrew L. Fraser, Eoin R. Gould, Elizabeth F. King, Stefanie K. Menzies, Joanne C. Morris, Marie I. Thomson, Lindsay B. Tulloch, Marija K. Zacharova, Terry K. Smith

Research output: Contribution to journalArticlepeer-review

10 Citations (Scopus)
64 Downloads (Pure)

Abstract

Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a burden to human and animal health, having the most devastating effect on the world's poorest countries. Building upon our previously reported triazole analogues, in this study we describe the synthesis and biological testing of other novel heterocyclic acetogenin-inspired derivatives, namely 3,5-isoxazoles, furoxans, and furazans. Several of these compounds maintain low-micromolar levels of inhibition against Trypanosoma brucei, whilst having no observable inhibitory effect on mammalian cells, leading to the possibility of novel lead compounds for selective treatment.

Original languageEnglish
Pages (from-to)1503-1506
Number of pages4
JournalChemMedChem
Volume11
Issue number14
Early online date10 Jun 2016
DOIs
Publication statusPublished - 19 Jul 2016

Keywords

  • Acetogenins/chemical synthesis
  • Cycloaddition Reaction
  • HeLa Cells
  • Humans
  • Isoxazoles/chemical synthesis
  • Oxadiazoles/chemical synthesis
  • Oximes/chemical synthesis
  • Trypanocidal Agents/chemical synthesis
  • Trypanosoma brucei brucei/drug effects

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