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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Detalles Bibliográficos
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
Descripción
Sumario: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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