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- W1990956558 abstract "A novel series of 6-(2-chloroquinolin-3-yl)-4-substituted-phenyl-6H-1,3-oxazin-2-amines were synthesized and evaluated for in vitro antimalarial efficacy against chloroquine sensitive (MRC-02) as well as chloroquine resistant (RKL9) strains of Plasmodium falciparum. The activity tested was at nanomolar concentration. β-Hematin formation inhibition activity (BHIA50) of oxazines were determined and correlated with antimalarial activity. A reasonably good correlation (r = 0.49 and 0.51, respectively) was observed between antimalarial activity (IC50) and BHIA50. This suggests that antimalarial mode of action of these compounds seems to be similar to that of chloroquine and involves the inhibition of hemozoin formation. Some of the compounds were showing better antimalarial activity than chloroquine against resistant strain of P. falciparum and were also found to be active in the in vivo experiment." @default.
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- W1990956558 date "2010-12-20" @default.
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- W1990956558 title "Novel oxazine skeletons as potential antiplasmodial active ingredients: Synthesis, <i>in vitro</i> and <i>in vivo</i> biology of some oxazine entities produced via cyclization of novel chalcone intermediates" @default.
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- W1990956558 doi "https://doi.org/10.3109/14756366.2010.539566" @default.
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