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

Authors: Charris, J. E.; Lobo, G. M.; Camacho, J.; Ferrer, R.; Barazarte, A.; Dominguez, J. N.; Gamboa, N.; Rodrigues, J. R.; Angel, J. E.

Source: Letters in Drug Design & Discovery, Volume 4, Number 1, January 2007 , pp. 49-54(6)

Publisher: Bentham Science Publishers

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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

Document Type: Research article

DOI: http://dx.doi.org/10.2174/157018007778992865

Affiliations: 1: Laboratorio de Síntesis Organica, Facultad de Farmacia, Universidad Central de Venezuela,Aptdo. 47206 Los Chaguaramos, 1041-A, Caracas, Venezuela.

Publication date: 2007-01-01

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