Abstract
Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC(50) value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimalarials / chemical synthesis
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Antimalarials / chemistry*
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Antimalarials / therapeutic use*
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Artemisinins / chemical synthesis
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Artemisinins / chemistry
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Artemisinins / therapeutic use
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Benzofurans / chemical synthesis
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Benzofurans / chemistry*
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Benzofurans / therapeutic use*
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Biological Products / chemical synthesis
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Biological Products / chemistry
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Biological Products / therapeutic use
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Cell Line
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Drug Discovery
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Female
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Malaria, Falciparum / drug therapy*
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Malaria, Falciparum / parasitology
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Mice
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Parasitic Sensitivity Tests
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Plasmodium falciparum / drug effects*
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Rats
Substances
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Antimalarials
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Artemisinins
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Benzofurans
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Biological Products
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usnic acid
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artenimol