Synthetic fosmidomycin analogues with altered chelating moieties do not inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase or Plasmodium falciparum growth in vitro

René Chofor, Martijn D P Risseeuw, Jenny Pouyez, Chinchu Johny, Johan Wouters, Cynthia S. Dowd, Robin D. Couch, Serge Van Calenbergh

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Résumé

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.

langue originaleAnglais
Pages (de - à)2571-2587
Nombre de pages17
journalMolecules
Volume19
Numéro de publication2
Les DOIs
Etat de la publicationPublié - 1 févr. 2014

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