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Letters in Drug Design & Discovery

Author(s): J. E. Charris, G. M. Lobo, J. Camacho, R. Ferrer, A. Barazarte, J. N. Dominguez, N. Gamboa, J. R. Rodrigues and J. E. Angel

DOI: 10.2174/157018007778992865

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Synthesis and Antimalarial Activity of (E) 2-(2-Chloro-3-Quinolinylmethylidene)-5,7-Dimethoxyindanones

Page: [49 - 54] Pages: 6

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Abstract

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