Abstract
A novel series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminacrine / chemical synthesis
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Aminacrine / chemistry
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / chemistry
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Antimalarials / pharmacology
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Artemisinins / chemical synthesis
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Artemisinins / chemistry
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Peroxides / chemical synthesis
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Peroxides / chemistry*
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Plasmodium falciparum / drug effects*
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology
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Structure-Activity Relationship
Substances
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Antimalarials
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Artemisinins
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Peroxides
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Quinolines
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Aminacrine
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artemisinin