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Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors

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

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Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors. / Fraser, Andrew L.; Menzies, Stefanie K.; King, Elizabeth F.B. et al.
In: ACS Infectious Diseases, Vol. 4, No. 4, 13.04.2018, p. 560-567.

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

Harvard

Fraser, AL, Menzies, SK, King, EFB, Tulloch, LB, Gould, ER, Zacharova, MK, Smith, TK & Florence, GJ 2018, 'Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors', ACS Infectious Diseases, vol. 4, no. 4, pp. 560-567. https://doi.org/10.1021/acsinfecdis.7b00187

APA

Fraser, A. L., Menzies, S. K., King, E. F. B., Tulloch, L. B., Gould, E. R., Zacharova, M. K., Smith, T. K., & Florence, G. J. (2018). Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors. ACS Infectious Diseases, 4(4), 560-567. https://doi.org/10.1021/acsinfecdis.7b00187

Vancouver

Fraser AL, Menzies SK, King EFB, Tulloch LB, Gould ER, Zacharova MK et al. Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors. ACS Infectious Diseases. 2018 Apr 13;4(4):560-567. doi: 10.1021/acsinfecdis.7b00187

Author

Fraser, Andrew L. ; Menzies, Stefanie K. ; King, Elizabeth F.B. et al. / Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors. In: ACS Infectious Diseases. 2018 ; Vol. 4, No. 4. pp. 560-567.

Bibtex

@article{0a582c0ead2c4102bec98b6464542d00,
title = "Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors",
abstract = "Neglected 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 photoaffinity probes capable of labeling target protein(s) in vitro. Several of these functionalized compounds maintain low micromolar activity against Trypanosoma brucei, Trypanosoma cruzi, Leishmania major, and Leishmania donovani. In addition, we demonstrate the utility of the photoaffinity probes for target identification through preliminary cellular localization studies.",
keywords = "chemical tools, drug design, natural products, photoaffinity, trypanosomatid",
author = "Fraser, {Andrew L.} and Menzies, {Stefanie K.} and King, {Elizabeth F.B.} and Tulloch, {Lindsay B.} and Gould, {Eoin R.} and Zacharova, {Marija K.} and Smith, {Terry K.} and Florence, {Gordon J.}",
year = "2018",
month = apr,
day = "13",
doi = "10.1021/acsinfecdis.7b00187",
language = "English",
volume = "4",
pages = "560--567",
journal = "ACS Infectious Diseases",
issn = "2373-8227",
publisher = "American Chemical Society",
number = "4",

}

RIS

TY - JOUR

T1 - Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors

AU - Fraser, Andrew L.

AU - Menzies, Stefanie K.

AU - King, Elizabeth F.B.

AU - Tulloch, Lindsay B.

AU - Gould, Eoin R.

AU - Zacharova, Marija K.

AU - Smith, Terry K.

AU - Florence, Gordon J.

PY - 2018/4/13

Y1 - 2018/4/13

N2 - Neglected 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 photoaffinity probes capable of labeling target protein(s) in vitro. Several of these functionalized compounds maintain low micromolar activity against Trypanosoma brucei, Trypanosoma cruzi, Leishmania major, and Leishmania donovani. In addition, we demonstrate the utility of the photoaffinity probes for target identification through preliminary cellular localization studies.

AB - Neglected 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 photoaffinity probes capable of labeling target protein(s) in vitro. Several of these functionalized compounds maintain low micromolar activity against Trypanosoma brucei, Trypanosoma cruzi, Leishmania major, and Leishmania donovani. In addition, we demonstrate the utility of the photoaffinity probes for target identification through preliminary cellular localization studies.

KW - chemical tools

KW - drug design

KW - natural products

KW - photoaffinity

KW - trypanosomatid

U2 - 10.1021/acsinfecdis.7b00187

DO - 10.1021/acsinfecdis.7b00187

M3 - Journal article

C2 - 29313667

AN - SCOPUS:85045314344

VL - 4

SP - 560

EP - 567

JO - ACS Infectious Diseases

JF - ACS Infectious Diseases

SN - 2373-8227

IS - 4

ER -