Abstract
In search of new 4-aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activities. Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro model with an IC(50) of 6.07ng/mL and also showed an in vivo suppression of 99.27% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminoquinolines / chemistry*
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / pharmacology
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Chemistry, Pharmaceutical / methods
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Chlorocebus aethiops
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Chloroquine / pharmacology
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Drug Design
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Drug Resistance
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Humans
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Inhibitory Concentration 50
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Plasmodium falciparum / metabolism
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Plasmodium yoelii / metabolism
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Thiazolidinediones / chemistry*
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Thiourea / analogs & derivatives*
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Thiourea / chemistry
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Vero Cells
Substances
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Aminoquinolines
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Antimalarials
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Thiazolidinediones
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Chloroquine
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2,4-thiazolidinedione
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4-aminoquinoline
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Thiourea