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 revueArticle

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
étatPublié - 1 févr. 2014

Empreinte digitale

Plasmodium falciparum
Chelation
enzymes
phosphates
analogs
tuberculosis
Plasmodium
erythrocytes
Enzymes
Growth
Escherichia coli
Tuberculosis
Erythrocytes
Metals
Ligands
ligands
metals
In Vitro Techniques
fosmidomycin
xylulose-5-phosphate

Citer ceci

Chofor, René ; Risseeuw, Martijn D P ; Pouyez, Jenny ; Johny, Chinchu ; Wouters, Johan ; Dowd, Cynthia S. ; Couch, Robin D. ; Van Calenbergh, Serge. / Synthetic fosmidomycin analogues with altered chelating moieties do not inhibit 1-deoxy-d-xylulose 5-phosphate reductoisomerase or Plasmodium falciparum growth in vitro. Dans: Molecules. 2014 ; Vol 19, Numéro 2. p. 2571-2587.
@article{b66c11c1655d435f8466a7fae53bb33d,
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 = "2",
day = "1",
doi = "10.3390/molecules19022571",
language = "English",
volume = "19",
pages = "2571--2587",
journal = "Molecules",
issn = "1431-5165",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "2",

}

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; Johny, Chinchu; Wouters, Johan; Dowd, Cynthia S.; Couch, Robin D.; Van Calenbergh, Serge.

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

Résultats de recherche: Contribution à un journal/une revueArticle

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

UR - http://www.scopus.com/inward/record.url?scp=84894618727&partnerID=8YFLogxK

U2 - 10.3390/molecules19022571

DO - 10.3390/molecules19022571

M3 - Article

AN - SCOPUS:84894618727

VL - 19

SP - 2571

EP - 2587

JO - Molecules

JF - Molecules

SN - 1431-5165

IS - 2

ER -