Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 21, Issue 8, Pages 1780-1784Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-011-9694-1
Keywords
Antimalarial; Chalcones; Coumarin
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Funding
- AICTE, New Delhi
- CSIR, New Delhi
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A novel series of 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4-nitrophenyl)acryloyl)-2H-chromen-2-one showed inhibitory potency (IC50) of 3.1 and 4 mu g/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance.
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