MedChemComm, volume 2, issue 9, pages 895
N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors
1
Active Biotech AB, PO Box 724, Lund, Sweden
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Publication type: Journal Article
Publication date: 2011-07-22
Journal:
MedChemComm
Quartile SCImago
— Quartile WOS
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SJR: —
CiteScore: —
Impact factor: —
ISSN: 20402503, 20402511
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.
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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.
Cite this
RIS
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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
PB - Royal Society of Chemistry (RSC)
SP - 895
IS - 9
VL - 2
SN - 2040-2503
SN - 2040-2511
ER -
Cite this
BibTex
Copy
@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
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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.