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

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

Volume: 4 Issue: 1

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

Affiliation:

Keywords: Malaria, Quinoline, Indanone, β-Hematin, P. berghei

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.

Cite this article as:

Charris E. J., Lobo M. G., Camacho J., Ferrer R., Barazarte A., Dominguez N. J., Gamboa N., Rodrigues R. J. and Angel E. J., Synthesis and Antimalarial Activity of (E) 2-(2-Chloro-3-Quinolinylmethylidene)-5,7-Dimethoxyindanones, Letters in Drug Design & Discovery 2007; 4 (1) . https://dx.doi.org/10.2174/157018007778992865