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In vitro activities of 2,4-diaminoquinazoline and 2,4-diaminopteridine derivatives against Plasmodium falciparum

Abstract:

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 50s) 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 IC50 of 9 nM. The activity of compound 1 was potentiated by the dihydropteroate synthase inhibitor dapsone, an indication that t...

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Publication status:
Published

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Authors


Kokwaro, G More by this author
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Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Tropical Medicine
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Journal:
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Volume:
48
Issue:
10
Pages:
3711-3714
Publication date:
2004-10-05
DOI:
EISSN:
1098-6596
ISSN:
0066-4804
URN:
uuid:3ab899bb-fd39-4fb8-8f12-943c369db7d7
Source identifiers:
39180
Local pid:
pubs:39180
Language:
English

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