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N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors

Författare

Summary, in English

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.

Publiceringsår

2011

Språk

Engelska

Sidor

895-898

Publikation/Tidskrift/Serie

MedChemComm

Volym

2

Issue

9

Dokumenttyp

Artikel i tidskrift

Förlag

Royal Society of Chemistry

Ämne

  • Medicinal Chemistry

Status

Published

ISBN/ISSN/Övrigt

  • ISSN: 2040-2511