Abstract
The synthesis and in-vitro antimalarial activity of gamma-substituted bis(pivaloyloxymethyl)ester analogues of the drug candidate fosmidomycin have been investigated. In contrast to the high antimalarial activity of alpha-aryl substituted fosmidomycin analogues like alpha-phenylfosmidomycin, gamma-substituted derivatives display only weak to moderate activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum.
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 / pharmacology*
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Esters
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Fosfomycin / analogs & derivatives*
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Fosfomycin / chemical synthesis
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Fosfomycin / chemistry
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Fosfomycin / pharmacology
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Humans
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Parasitic Sensitivity Tests
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Plasmodium falciparum / drug effects
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Structure-Activity Relationship
Substances
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Antimalarials
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Esters
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Fosfomycin
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fosmidomycin
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3-(N-acetyl-N-hydroxy)aminopropylphosphonic acid