N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors

Ingela Fritzson, Paul T. P. Bedingfield, Anders Sundin, Glenn McConkey, Ulf Nilsson

Research output: Contribution to journalArticlepeer-review

10 Citations (SciVal)

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.
Original languageEnglish
Pages (from-to)895-898
JournalMedChemComm
Volume2
Issue number9
DOIs
Publication statusPublished - 2011

Bibliographical note

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)

Subject classification (UKÄ)

  • Medicinal Chemistry

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