Synthesis and Antimalarial Activity of (E) 2-(2-Chloro-3-Quinolinylmethylidene)-5,7-Dimethoxyindanones
J. E. Charris,
G. M. Lobo,
J. N. Dominguez,
J. R. Rodrigues,
J. E. Angel.
A series of (E) 2-quinolinylmethylidene-5,7-dimethoxyindanones were prepared via base catalyzed Claisen-Schmidt condensation of 5,7-dimethoxy-1-indanone with the appropriate 2-chloro-3-formylquinoline derivative. Evaluation of their in vitro inhibition of β-hematin formation and hemoglobin hydrolysis and in vivo efficacy in rodent Plasmodium berghei suggest the antimalarial activity is derived from inhibition of hemoglobinolytic proteases.
Keywords: Malaria, Quinoline, Indanone, β-Hematin, P. berghei
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