Abstract
Selected members of three classes of rhodacyanine dyes, [0,0]-, [1,0]-, and [0,0,0]-rhodacyanines, were synthesized and their in vitro antimalarial activities against Plasmodium falciparum K1 (chloroquine-resistant strain) as well as their in vivo activities against P. berghei in mice were determined. The novel [0,0,0]-rhodacynines, 3e and 3h, possessing a benzothiazole moiety, were shown to have highly promising antimalarial activities in vivo. Moreover, the [0,0,0]-rhodacyanines were found to be orally bioavailable.
Publication types
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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 / pharmacology
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Cells, Cultured
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Chloroquine / adverse effects
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Coloring Agents / chemical synthesis*
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Coloring Agents / pharmacology
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Drug Resistance
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Malaria, Falciparum / drug therapy*
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Malaria, Falciparum / parasitology
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Male
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Mice
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Mice, Inbred ICR
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Myoblasts, Skeletal / drug effects
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Plasmodium berghei / drug effects*
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Plasmodium falciparum / drug effects*
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Pyridinium Compounds / chemical synthesis*
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Pyridinium Compounds / pharmacology
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Rats
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
Substances
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Antimalarials
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Coloring Agents
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Pyridinium Compounds
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Thiazoles
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rhodacyanine
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Chloroquine