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Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors

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Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors. / Florence, Gordon J.; Fraser, Andrew L.; Gould, Eoin R. et al.
In: ChemMedChem, Vol. 11, No. 14, 19.07.2016, p. 1503-1506.

Research output: Contribution to Journal/Magazine › Journal article › peer-review

Harvard

Florence, GJ, Fraser, AL, Gould, ER, King, EF, Menzies, SK, Morris, JC, Thomson, MI, Tulloch, LB, Zacharova, MK & Smith, TK 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.201600210

APA

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, 11(14), 1503-1506. https://doi.org/10.1002/cmdc.201600210

Vancouver

Florence GJ, Fraser AL, Gould ER, King EF, Menzies SK, Morris JC et al. Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors. ChemMedChem. 2016 Jul 19;11(14):1503-1506. Epub 2016 Jun 10. doi: 10.1002/cmdc.201600210

Author

Florence, Gordon J. ; Fraser, Andrew L. ; Gould, Eoin R. et al. / Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors. In: ChemMedChem. 2016 ; Vol. 11, No. 14. pp. 1503-1506.

Bibtex

@article{7bf75dadd1b6463cae8a4f7c8dda3aba,
title = "Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors",
abstract = "Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a 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.",
keywords = "drug discovery, natural product analogues, trypanosomatids, [3+2] cycloaddition",
author = "Florence, {Gordon J.} and Fraser, {Andrew L.} and Gould, {Eoin R.} and King, {Elizabeth F.} and Menzies, {Stefanie K.} and Morris, {Joanne C.} and Thomson, {Marie I.} and Tulloch, {Lindsay B.} and Zacharova, {Marija K.} and Smith, {Terry K.}",
note = "Publisher Copyright: {\textcopyright} 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim",
year = "2016",
month = jul,
day = "19",
doi = "10.1002/cmdc.201600210",
language = "English",
volume = "11",
pages = "1503--1506",
journal = "ChemMedChem",
issn = "1860-7179",
publisher = "John Wiley and Sons Ltd",
number = "14",

}

RIS

TY - JOUR

T1 - Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors

AU - Florence, Gordon J.

AU - Fraser, Andrew L.

AU - Gould, Eoin R.

AU - King, Elizabeth F.

AU - Menzies, Stefanie K.

AU - Morris, Joanne C.

AU - Thomson, Marie I.

AU - Tulloch, Lindsay B.

AU - Zacharova, Marija K.

AU - Smith, Terry K.

N1 - Publisher Copyright: © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim

PY - 2016/7/19

Y1 - 2016/7/19

N2 - Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a 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.

AB - Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a 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.

KW - drug discovery

KW - natural product analogues

KW - trypanosomatids

KW - [3+2] cycloaddition

U2 - 10.1002/cmdc.201600210

DO - 10.1002/cmdc.201600210

M3 - Journal article

C2 - 27283448

AN - SCOPUS:84978763282

VL - 11

SP - 1503

EP - 1506

JO - ChemMedChem

JF - ChemMedChem

SN - 1860-7179

IS - 14

ER -