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Wiley, ChemMedChem, 11(9), p. 2548-2556, 2014

DOI: 10.1002/cmdc.201402272

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Non-natural acetogenin analogues as potent Trypanosoma brucei inhibitors

Journal article published in 2014 by Gordon J. Florence, Andrew L. Fraser, Eoin R. Gould, Elizabeth F. B. King, Stefanie K. Menzies ORCID, Joanne C. Morris, Lindsay B. Tulloch, Terry K. Smith
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This paper is available in a repository.

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Abstract

A series of novel bis-tetrahydropyran 1,4-triazole analogues based on the acetogenin framework display low micromolar trypanocidal activities towards both bloodstream and insect forms of Trypanosoma brucei, the causative agent of African sleeping sickness. A divergent synthetic strategy was adopted for the synthesis of the key tetrahydropyran intermediates to enable rapid access to diastereochemical variation either side of the 1,4-triazole core. The resulting diastereomeric analogues displayed varying degrees of trypanocidal activity and selectivity in structure activity relationship studies.