Abstract
Sixteen antimalarial alkoxylated and hydroxylated chalcones were tested for their ability to inhibit recombinant plasmepsin II in vitro. The best inhibitory compounds had either a chloro or dimethylamino group at the 4-position of phenyl ring A in the chalcone template. Combination of the chalcones with chloroquine showed additivity or mild antagonism of Plasmodium falciparum K1 growth in culture.
MeSH terms
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Animals
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Antimalarials / pharmacology*
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Aspartic Acid Endopeptidases / antagonists & inhibitors*
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Chalcones / chemistry
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Chalcones / pharmacology*
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Chalcones / toxicity
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Chloroquine / toxicity*
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Inhibitory Concentration 50
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Molecular Structure
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Plasmodium falciparum / drug effects*
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Protozoan Proteins
Substances
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Antimalarials
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Chalcones
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Protozoan Proteins
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Chloroquine
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Aspartic Acid Endopeptidases
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plasmepsin II