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

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	2571-2587
Number of pages	17
Journal	Molecules
Volume	19
Issue number	2
DOIs	https://doi.org/10.3390/molecules19022571
Publication status	Published - 1 Feb 2014

Keywords

Coordination chemistry
DOXP reductoisomerase
Fosmidomycin
Isoprenoid biosynthesis
Non-mevalonate pathway

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3390/molecules19022571

Cite this

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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",

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doi = "10.3390/molecules19022571",

language = "English",

volume = "19",

pages = "2571--2587",

journal = "Molecules",

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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

M3 - Article

AN - SCOPUS:84894618727

SN - 1420-3049

VL - 19

SP - 2571

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

Abstract

Keywords

UN SDGs

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Physical Chemistry and characterization(PC2)

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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

Abstract

Keywords

UN SDGs

Access to Document

Other files and links

Embargoed Document

Fingerprint

Equipment

Physical Chemistry and characterization(PC2)

Cite this