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Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors
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...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5111590/ https://www.ncbi.nlm.nih.gov/pubmed/27283448 http://dx.doi.org/10.1002/cmdc.201600210 |
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author | Florence, Gordon J. Fraser, Andrew L. Gould, Eoin R. King, Elizabeth F. Menzies, Stefanie K. Morris, Joanne C. Thomson, Marie I. Tulloch, Lindsay B. Zacharova, Marija K. Smith, Terry K. |
author_facet | Florence, Gordon J. Fraser, Andrew L. Gould, Eoin R. King, Elizabeth F. Menzies, Stefanie K. Morris, Joanne C. Thomson, Marie I. Tulloch, Lindsay B. Zacharova, Marija K. Smith, Terry K. |
author_sort | Florence, Gordon J. |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-5111590 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-51115902016-11-16 Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors Florence, Gordon J. Fraser, Andrew L. Gould, Eoin R. King, Elizabeth F. Menzies, Stefanie K. Morris, Joanne C. Thomson, Marie I. Tulloch, Lindsay B. Zacharova, Marija K. Smith, Terry K. ChemMedChem Communications 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. John Wiley and Sons Inc. 2016-06-10 2016-07-19 /pmc/articles/PMC5111590/ /pubmed/27283448 http://dx.doi.org/10.1002/cmdc.201600210 Text en © 2016 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of the Creative Commons Attribution (http://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Communications Florence, Gordon J. Fraser, Andrew L. Gould, Eoin R. King, Elizabeth F. Menzies, Stefanie K. Morris, Joanne C. Thomson, Marie I. Tulloch, Lindsay B. Zacharova, Marija K. Smith, Terry K. Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors |
title | Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors |
title_full | Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors |
title_fullStr | Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors |
title_full_unstemmed | Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors |
title_short | Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors |
title_sort | development of simplified heterocyclic acetogenin analogues as potent and selective trypanosoma brucei inhibitors |
topic | Communications |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5111590/ https://www.ncbi.nlm.nih.gov/pubmed/27283448 http://dx.doi.org/10.1002/cmdc.201600210 |
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