Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro

Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. T...

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Autores principales: Chofor, René, Risseeuw, Martijn D.P., Pouyez, Jenny, Johny, Chinchu, Wouters, Johan, Dowd, Cynthia S., Couch, Robin D., Van Calenbergh, Serge
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271069/
https://www.ncbi.nlm.nih.gov/pubmed/24566322
http://dx.doi.org/10.3390/molecules19022571
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author Chofor, René
Risseeuw, Martijn D.P.
Pouyez, Jenny
Johny, Chinchu
Wouters, Johan
Dowd, Cynthia S.
Couch, Robin D.
Van Calenbergh, Serge
author_facet Chofor, René
Risseeuw, Martijn D.P.
Pouyez, Jenny
Johny, Chinchu
Wouters, Johan
Dowd, Cynthia S.
Couch, Robin D.
Van Calenbergh, Serge
author_sort Chofor, René
collection PubMed
description Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. This study further underlines the importance of the hydroxamate functionality and illustrates that identifying effective alternative bidentate ligands for this target enzyme is challenging.
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spelling pubmed-62710692018-12-20 Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro Chofor, René Risseeuw, Martijn D.P. Pouyez, Jenny Johny, Chinchu Wouters, Johan Dowd, Cynthia S. Couch, Robin D. Van Calenbergh, Serge Molecules Article Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. This study further underlines the importance of the hydroxamate functionality and illustrates that identifying effective alternative bidentate ligands for this target enzyme is challenging. MDPI 2014-02-24 /pmc/articles/PMC6271069/ /pubmed/24566322 http://dx.doi.org/10.3390/molecules19022571 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Chofor, René
Risseeuw, Martijn D.P.
Pouyez, Jenny
Johny, Chinchu
Wouters, Johan
Dowd, Cynthia S.
Couch, Robin D.
Van Calenbergh, Serge
Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
title Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
title_full Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
title_fullStr Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
title_full_unstemmed Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
title_short Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-d-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
title_sort synthetic fosmidomycin analogues with altered chelating moieties do not inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase or plasmodium falciparum growth in vitro
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271069/
https://www.ncbi.nlm.nih.gov/pubmed/24566322
http://dx.doi.org/10.3390/molecules19022571
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