Abstract
The antimalarial acitivity of hydroxyethylamines, synthesized from the reaction of intermediated hydroxyethypiperazines with benzenesulfonyl chlorides or benzoyl chlorides, has been evaluated in vitro against a W2 Plasmodium falciparum clone. Some of the nineteen tested derivatives showed a significant activity in vitro, thus turning into a promising new class of antimalarials. In addition, a molecular modeling study of the most active derivative (5l) was performed and its most probable binding modes within plasmepsin II enzyme were identified.
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 / chemistry*
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Antimalarials / pharmacology*
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Antimalarials / toxicity
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Aspartic Acid Endopeptidases / metabolism
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Cell Line
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Erythrocytes / parasitology
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Ethanolamines / chemical synthesis*
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Ethanolamines / chemistry
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Ethanolamines / pharmacology*
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Ethanolamines / toxicity
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Humans
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Macrophages / cytology
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Macrophages / drug effects
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Malaria, Falciparum / drug therapy*
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Models, Molecular
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Monocytes / cytology
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Monocytes / drug effects
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Murinae
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Plasmodium falciparum / drug effects*
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Plasmodium falciparum / enzymology
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Protein Binding
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Protozoan Proteins / metabolism
Substances
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Antimalarials
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Ethanolamines
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Protozoan Proteins
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Aspartic Acid Endopeptidases
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plasmepsin II