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The activities of 28 6-substituted 2,4-diaminoquinazolines, 2,4-diamino-5,6,7,8-tetrahydroquinazolines, and 2,4-diaminopteridines against Plasmodium falciparum were tested. The 50% inhibitory concentrations (IC(50)s) of six compounds were <50 nM, and the most potent compound was 2,4-diamino-5-chloro-6-[N-(2,5-dimethoxybenzyl)amino]quinazoline (compound 1), with an IC(50) of 9 nM. The activity of compound 1 was potentiated by the dihydropteroate synthase inhibitor dapsone, an indication that these compounds are inhibitors of dihydrofolate reductase. Further studies are warranted to assess the therapeutic potential of this combination in vivo.

Original publication

DOI

10.1128/AAC.48.10.3711-3714.2004

Type

Journal

Antimicrobial agents and chemotherapy

Publication Date

10/2004

Volume

48

Pages

3711 - 3714

Addresses

Kenya Medical Research Institute (KEMRI)/Wellcome Trust Collaborative Research Program, Wellcome Trust Research Laboratories, P.O. Box 43640 GPO, 00100 Nairobi, Kenya. anzila@wtnairobi.mimcom.net

Keywords

Animals, Plasmodium falciparum, Saccharomyces cerevisiae, Dapsone, Pteridines, Quinazolines, Tetrahydrofolate Dehydrogenase, Dihydropteroate Synthase, Folic Acid Antagonists, Antimalarials, Drug Resistance