Abstract
A convenient route to N-substituted bis-C-alkylamidines possessing antiplasmodial activity and their oxadiazolone and amidoxime prodrug candidates, is described. These three families of compounds were available after a key N-alkylation step of the parent oxadiazolone 1a. Testing of the three compound classes in vitro and in vivo is also presented.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amidines / chemical synthesis
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Amidines / chemistry*
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Amidines / pharmacology
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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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Female
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Mice
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Oxadiazoles / chemical synthesis
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Oxadiazoles / chemistry*
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Oxadiazoles / pharmacology
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Oximes / chemical synthesis
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Oximes / chemistry*
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Oximes / pharmacology
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Plasmodium / drug effects
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Prodrugs / chemical synthesis
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Prodrugs / chemistry*
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Prodrugs / pharmacology
Substances
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Amidines
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Antimalarials
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Oxadiazoles
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Oximes
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Prodrugs