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dc.contributor.authorFlorence, Gordon J.
dc.contributor.authorFraser, Andrew L.
dc.contributor.authorGould, Eoin R.
dc.contributor.authorKing, Elizabeth F.
dc.contributor.authorMenzies, Stefanie K.
dc.contributor.authorMorris, Joanne C.
dc.contributor.authorThomson, Marie I.
dc.contributor.authorTulloch, Lindsay B.
dc.contributor.authorZacharova, Marija K.
dc.contributor.authorSmith, Terry K.
dc.date.accessioned2017-06-10T23:33:30Z
dc.date.available2017-06-10T23:33:30Z
dc.date.issued2016-07-19
dc.identifier.citationFlorence , G J , Fraser , A L , Gould , E R , King , E F , Menzies , S K , Morris , J C , Thomson , M I , Tulloch , L B , Zacharova , M K & Smith , T K 2016 , ' Development of simplified heterocyclic acetogenin analogues as potent and selective Trypanosoma brucei inhibitors ' ChemMedChem , vol. 11 , no. 14 , pp. 1503-1506 . https://doi.org/10.1002/cmdc.201600210en
dc.identifier.issn1860-7179
dc.identifier.otherPURE: 241712299
dc.identifier.otherPURE UUID: 6a1ae42a-9a93-4f5e-bdd5-9144a9a82588
dc.identifier.otherScopus: 84978763282
dc.identifier.otherORCID: /0000-0002-8987-5561/work/27750839
dc.identifier.otherORCID: /0000-0001-7223-5106/work/42522363
dc.identifier.otherORCID: /0000-0001-9921-4399/work/56638871
dc.identifier.urihttp://hdl.handle.net/10023/10977
dc.descriptionThis work was funded by the Leverhulme Trust (GJF), and the Wellcome Trust (TKS, WT 093228).en
dc.description.abstractNeglected tropical diseases caused by parasitic infections are an on-going and increasing concern and 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.
dc.format.extent4
dc.language.isoeng
dc.relation.ispartofChemMedChemen
dc.rights© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. This work is made available online in accordance with the publisher’s policies. This is the author created, accepted version manuscript following peer review and may differ slightly from the final published version. The final published version of this work is available at https://dx.doi.org/10.1002/cmdc.201600210en
dc.subject[3+2] cycloadditionen
dc.subjectDrug discoveryen
dc.subjectNatural product analoguesen
dc.subjectTrypanosomatidsen
dc.subjectQD Chemistryen
dc.subjectNDASen
dc.subject.lccQDen
dc.titleDevelopment of simplified heterocyclic acetogenin analogues as potent and selective Trypanosoma brucei inhibitorsen
dc.typeJournal itemen
dc.description.versionPostprinten
dc.contributor.institutionUniversity of St Andrews.School of Chemistryen
dc.contributor.institutionUniversity of St Andrews.Biomedical Sciences Research Complexen
dc.contributor.institutionUniversity of St Andrews.EaSTCHEMen
dc.contributor.institutionUniversity of St Andrews.School of Biologyen
dc.identifier.doihttps://doi.org/10.1002/cmdc.201600210
dc.description.statusPeer revieweden
dc.date.embargoedUntil2017-06-10


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