Abstract
A novel cytotoxin 3,5-bis(4-chlorobenzylidene)-1-[4-{2-(4-morpholinyl)ethoxy}phenyl-carbonyl]-4-piperidone hydrochloride 2 demonstrated potent antimalarial properties with IC(50) values of 0.60 and 1.97 μM against the drug sensitive D6 strain and the C235 drug-resistant strain of Plasmodium falciparum. This compound concentrates in red blood cells, lowers glutathione concentrations in erythrocytes and permeates across CACO-2 cells. These data reveal 2 to be a promising lead compound in the quest for novel antimalarial agents.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antimalarials / chemical synthesis*
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Antimalarials / chemistry
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Antimalarials / pharmacology
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Caco-2 Cells
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Drug Discovery*
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Drug Resistance
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Humans
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Inhibitory Concentration 50
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Morpholines / chemical synthesis*
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Morpholines / chemistry
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Morpholines / pharmacology
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Piperidones / chemical synthesis*
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Piperidones / chemistry
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Piperidones / pharmacology
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Plasmodium falciparum / drug effects
Substances
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3,5-bis(4-chlorobenzylidene)-1-(4-(2-(4-morpholinyl)ethoxy)phenyl-carbonyl)-4-piperidone
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Antimalarials
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Morpholines
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Piperidones