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Molecules 2014, 19(2), 2571-2587; doi:10.3390/molecules19022571
Article

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

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Received: 6 February 2014 / Revised: 18 February 2014 / Accepted: 19 February 2014 / Published: 24 February 2014
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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.
Keywords: fosmidomycin; DOXP reductoisomerase; non-mevalonate pathway; isoprenoid biosynthesis; coordination chemistry fosmidomycin; DOXP reductoisomerase; non-mevalonate pathway; isoprenoid biosynthesis; coordination chemistry
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Chofor, R.; Risseeuw, M.D.; Pouyez, J.; Johny, C.; Wouters, J.; Dowd, C.S.; Couch, R.D.; Van Calenbergh, S. Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-D-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro. Molecules 2014, 19, 2571-2587.

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