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

doi:10.3390/molecules19022571

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

Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

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 originale	Anglais
Pages (de - à)	2571-2587
Nombre de pages	17
journal	Molecules
Volume	19
Numéro de publication	2
Les DOIs	https://doi.org/10.3390/molecules19022571
Etat de la publication	Publié - 1 févr. 2014

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10.3390/molecules19022571

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

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 = "Coordination chemistry, DOXP reductoisomerase, Fosmidomycin, Isoprenoid biosynthesis, Non-mevalonate pathway",

author = "Ren{\'e} Chofor and Risseeuw, {Martijn D P} and Jenny Pouyez and Chinchu Johny and Johan Wouters and Dowd, {Cynthia S.} and Couch, {Robin D.} and {Van Calenbergh}, Serge",

year = "2014",

month = feb,

day = "1",

doi = "10.3390/molecules19022571",

language = "English",

volume = "19",

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journal = "Molecules",

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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 et al.
Dans: Molecules, Vol 19, Numéro 2, 01.02.2014, p. 2571-2587.

Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

TY - JOUR

T1 - Synthetic fosmidomycin analogues with altered chelating moieties do not inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase or Plasmodium falciparum growth in vitro

AU - Chofor, René

AU - Risseeuw, Martijn D P

AU - Pouyez, Jenny

AU - Johny, Chinchu

AU - Wouters, Johan

AU - Dowd, Cynthia S.

AU - Couch, Robin D.

AU - Van Calenbergh, Serge

PY - 2014/2/1

Y1 - 2014/2/1

N2 - 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.

AB - 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.

KW - Coordination chemistry

KW - DOXP reductoisomerase

KW - Fosmidomycin

KW - Isoprenoid biosynthesis

KW - Non-mevalonate pathway

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DO - 10.3390/molecules19022571

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VL - 19

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EP - 2587

JO - Molecules

JF - Molecules

IS - 2

ER -

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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