MedChemComm, volume 2, issue 9, pages 895
N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors
Ingela Fritzson
1, 2
,
Paul T P Bedingfield
3
,
ANDERS SUNDIN
2
,
Glenn A. McConkey
3
,
Ulf Nilsson
2
1
Active Biotech AB, PO Box 724, Lund, Sweden
|
Publication type: Journal Article
Publication date: 2011-07-22
Organic Chemistry
Drug Discovery
Biochemistry
Pharmacology
Pharmaceutical Science
Molecular Medicine
Abstract
In our continuing program to develop Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors, a series of N-substituted salicylamides were synthesized and their ability to selectively inhibit PfDHODH was examined. The synthetic program was based on 2-hydroxy-N-(2-phenylethyl)benzamide (1) that weakly inhibits both PfDHODH and human DHODH (hDHODH). Structure activity relationships were examined for developing derivatives. Selective PfDHODH inhibitors with improved potency were obtained by introducing a 2,2-diphenylethyl substitution on the salicylamidic nitrogen. Biological activity of the most potent compounds was confirmed on parasite infected cells in vitro.
Top-30
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1 publication, 5.88%
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1 publication, 5.88%
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1 publication, 5.88%
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Citations by publishers
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1
2
3
4
5
6
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Elsevier
6 publications, 35.29%
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2 publications, 11.76%
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2 publications, 11.76%
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1 publication, 5.88%
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Portland Press
1 publication, 5.88%
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Wiley
1 publication, 5.88%
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American Chemical Society (ACS)
1 publication, 5.88%
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Royal Society of Chemistry (RSC)
1 publication, 5.88%
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Springer Nature
1 publication, 5.88%
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Autonomous Non-profit Organization Editorial Board of the journal Uspekhi Khimii
1 publication, 5.88%
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- We do not take into account publications without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Fritzson I. et al. N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors // MedChemComm. 2011. Vol. 2. No. 9. p. 895.
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Fritzson I., Bedingfield P. T. P., SUNDIN A., McConkey G. A., Nilsson U. N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors // MedChemComm. 2011. Vol. 2. No. 9. p. 895.
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TY - JOUR
DO - 10.1039/c1md00118c
UR - https://doi.org/10.1039/c1md00118c
TI - N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors
T2 - MedChemComm
AU - Fritzson, Ingela
AU - Bedingfield, Paul T P
AU - SUNDIN, ANDERS
AU - McConkey, Glenn A.
AU - Nilsson, Ulf
PY - 2011
DA - 2011/07/22 00:00:00
PB - Royal Society of Chemistry (RSC)
SP - 895
IS - 9
VL - 2
SN - 2040-2503
SN - 2040-2511
ER -
Cite this
BibTex
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@article{2011_Fritzson,
author = {Ingela Fritzson and Paul T P Bedingfield and ANDERS SUNDIN and Glenn A. McConkey and Ulf Nilsson},
title = {N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors},
journal = {MedChemComm},
year = {2011},
volume = {2},
publisher = {Royal Society of Chemistry (RSC)},
month = {jul},
url = {https://doi.org/10.1039/c1md00118c},
number = {9},
pages = {895},
doi = {10.1039/c1md00118c}
}
Cite this
MLA
Copy
Fritzson, Ingela, et al. “N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors.” MedChemComm, vol. 2, no. 9, Jul. 2011, p. 895. https://doi.org/10.1039/c1md00118c.