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N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors

Fritzson, Ingela LU ; Bedingfield, Paul T. P. ; Sundin, Anders LU ; McConkey, Glenn and Nilsson, Ulf LU (2011) In MedChemComm 2(9). p.895-898
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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author
; ; ; and
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
MedChemComm
volume
2
issue
9
pages
895 - 898
publisher
Royal Society of Chemistry
external identifiers
  • wos:000295710300012
  • scopus:80052363272
ISSN
2040-2511
DOI
10.1039/c1md00118c
language
English
LU publication?
yes
additional info
The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)
id
dea89224-b79b-4e71-8f5d-3ac1cca0d179 (old id 2212662)
date added to LUP
2016-04-01 10:02:06
date last changed
2025-04-04 14:10:43
@article{dea89224-b79b-4e71-8f5d-3ac1cca0d179,
  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.}},
  author       = {{Fritzson, Ingela and Bedingfield, Paul T. P. and Sundin, Anders and McConkey, Glenn and Nilsson, Ulf}},
  issn         = {{2040-2511}},
  language     = {{eng}},
  number       = {{9}},
  pages        = {{895--898}},
  publisher    = {{Royal Society of Chemistry}},
  series       = {{MedChemComm}},
  title        = {{N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors}},
  url          = {{http://dx.doi.org/10.1039/c1md00118c}},
  doi          = {{10.1039/c1md00118c}},
  volume       = {{2}},
  year         = {{2011}},
}