Development of simplified heterocyclic acetogenin analogues as potent and selective Trypanosoma brucei inhibitors
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Neglected 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.
Florence , 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 . DOI: 10.1002/cmdc.201600210
© 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.201600210
DescriptionThis work was funded by the Leverhulme Trust (GJF), and the Wellcome Trust (TKS, WT 093228).
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