In vitro activities of 2,4-diaminoquinazoline and 2,4-diaminopteridine derivatives against Plasmodium falciparum
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Date
2004Author
Ommeh, S
Nduati, E
Mberu, E
Kokwaro, G
Marsh, K
Rosowsky, A
Nzila, A
Type
ArticleLanguage
enMetadata
Show full item recordAbstract
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
URI
http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/31034http://www.ncbi.nlm.nih.gov/pubmed/15388424
Citation
Antimicrob Agents Chemother. 2004 Oct;48(10):3711-4Publisher
University of Nairobi School of Medicine
Collections
- Faculty of Health Sciences (FHS) [10377]