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Design and synthesis of broad spectrum trypanosomatid selective inhibitors

Research output: Research - peer-reviewArticle

DOI

Author(s)

Andrew L. Fraser, Stefanie K. Menzies, Elizabeth F. B. King, Lindsay Tulloch, Eoin R. Gould, Marija Zacharova, Terry K. Smith, Gordon J. Florence

School/Research organisations

Abstract

Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern that have a devastating effect on the developing world due to their burden on human and animal health. In this work, we detail the preparation of a focused library of substituted-tetrahydropyran derivatives and their evaluation as selective chemical tools for trypanosomatid inhibition and the follow-on development of photo-affinity probes capable of labeling target protein(s) in vitro. Several of these functionalised compounds maintain low micromolar activity against Trypanosoma brucei, Trypanosoma cruzi, Leishmania major and Leishmania donovani. In addition we demonstrate the utility of the photo-affinity probes for target identification through preliminary cellular localization studies.
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Original languageEnglish
Pages (from-to)560-567
Number of pages8
JournalACS Infectious Diseases
Volume4
Issue number4
Early online date9 Jan 2018
DOIs
StatePublished - 13 Apr 2018

    Research areas

  • Trypanosomatid, Natural Products, Drug Design, Chemical Tools, Photo-affinity

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