Abstract
A series of 1H-1,2,3-triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates have been synthesized and evaluated for their antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum. The most potent of the test compound with an optimum combination of 3-hydroxy-indole ring and a n-butyl linker displayed an IC50 value of 69 nM.
Keywords:
1H-1,2,3-Triazole; 3-Hydroxy-indole-2-one; 7-Chloroquinoline; Antimalarial activity; Isatin.
Copyright © 2013 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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Chloroquine / chemical synthesis
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Chloroquine / chemistry
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Chloroquine / pharmacology
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Drug Resistance
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Hydrazines / chemical synthesis*
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Hydrazines / chemistry
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Hydrazines / pharmacology*
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology
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Inhibitory Concentration 50
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Isatin / chemical synthesis
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Isatin / chemistry
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Isatin / pharmacology
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Plasmodium falciparum / drug effects*
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology*
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Structure-Activity Relationship
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Triazoles / chemical synthesis
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Triazoles / chemistry
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Triazoles / pharmacology
Substances
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Antimalarials
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Hydrazines
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Indoles
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Quinolines
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Triazoles
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Isatin
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indole
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Chloroquine