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dc.contributor.authorFraser, Andrew L.
dc.contributor.authorMenzies, Stefanie K.
dc.contributor.authorKing, Elizabeth F. B.
dc.contributor.authorTulloch, Lindsay
dc.contributor.authorGould, Eoin R.
dc.contributor.authorZacharova, Marija
dc.contributor.authorSmith, Terry K.
dc.contributor.authorFlorence, Gordon J.
dc.identifier.citationFraser , A L , Menzies , S K , King , E F B , Tulloch , L , Gould , E R , Zacharova , M , Smith , T K & Florence , G J 2018 , ' Design and synthesis of broad spectrum trypanosomatid selective inhibitors ' , ACS Infectious Diseases , vol. 4 , no. 4 , pp. 560-567 .
dc.identifier.otherPURE: 246494357
dc.identifier.otherPURE UUID: 91d55cba-4bf2-44ac-9d02-aeb5dd7d5e4d
dc.identifier.otherScopus: 85045314344
dc.identifier.otherORCID: /0000-0002-8987-5561/work/40797746
dc.identifier.otherORCID: /0000-0001-7223-5106/work/42522356
dc.identifier.otherORCID: /0000-0001-9921-4399/work/56638874
dc.identifier.otherWOS: 000430369900016
dc.descriptionThis work was funded by the Leverhulme Trust (GJF) and the European Community’s Seventh Framework Programme under grant agreement No. 602773 [Project KINDRED] (TKS).en
dc.description.abstractNeglected 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.
dc.relation.ispartofACS Infectious Diseasesen
dc.rightsCopyright © 2018 American Chemical Society. This work has been made available online in accordance with the publisher’s policies. This is the author created accepted version manuscript following peer review and as such may differ slightly from the final published version. The final published version of this work is available at:
dc.subjectNatural Productsen
dc.subjectDrug Designen
dc.subjectChemical Toolsen
dc.subjectQD Chemistryen
dc.subjectRM Therapeutics. Pharmacologyen
dc.subjectSDG 3 - Good Health and Well-beingen
dc.titleDesign and synthesis of broad spectrum trypanosomatid selective inhibitorsen
dc.typeJournal articleen
dc.contributor.sponsorThe Leverhulme Trusten
dc.contributor.sponsorEuropean Commissionen
dc.contributor.institutionUniversity of St Andrews. School of Chemistryen
dc.contributor.institutionUniversity of St Andrews. School of Biologyen
dc.contributor.institutionUniversity of St Andrews. Biomedical Sciences Research Complexen
dc.contributor.institutionUniversity of St Andrews. EaSTCHEMen
dc.description.statusPeer revieweden

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