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

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Pages (from-to)2571-2587
Number of pages17
JournalMolecules
Volume19
Issue number2
DOIs
Publication statusPublished - 1 Feb 2014

    Fingerprint

Keywords

  • Coordination chemistry
  • DOXP reductoisomerase
  • Fosmidomycin
  • Isoprenoid biosynthesis
  • Non-mevalonate pathway

Cite this