Abstract
We have developed the [5-(4-nitrophenyl)-2-furyl]acrylic acid substituted benzophenone 4g as a novel lead for anti-malarial agents. Here, we demonstrated that the acyl residue at the 2-amino group of the benzophenone core structure has to be a phenylacetic acid substructure substituted in its para-position with methyl or other substituents of similar size. The trifluoromethyl substituted derivative displayed an IC(50) of 47 nM against the multi-drug resistant Plasmodium falciparum strain Dd2.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acrylates / chemical synthesis*
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Acrylates / pharmacology
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / pharmacology
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Drug Resistance, Multiple
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Erythrocytes / drug effects
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Erythrocytes / parasitology
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Furans / chemical synthesis*
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Furans / pharmacology
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Humans
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Indicators and Reagents
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Plasmodium falciparum / drug effects
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Structure-Activity Relationship
Substances
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Acrylates
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Antimalarials
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Furans
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Indicators and Reagents
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N-(4-acylamino-3-benzoylphenyl)-(5-(4-nitrophenyl)-2-furyl)acrylic acid amide