Resumen

TORRES, Omar L; ESPINOSA, Roger D; SAEZ, Alex A  y  SANTAFE, Gilmar G. Evaluation of Antimalarial and Cytotoxic Activity of Styrylquinolines obtained from 8-Hydroxyquinaldine with Aromatic Aldehydes. Inf. tecnol. [online]. 2014, vol.25, n.6, pp.91-100. ISSN 0718-0764.  http://dx.doi.org/10.4067/S0718-07642014000600012.

This study reports the synthesis of five (E)-Styrylquinolines (Q.1, Q.2, Q.3, Q.5, Q.6) and three O-alkylated derivatives (Q.1a, Q.6a, Q 6 b) and the evaluation of its antimalarial activity and cytotoxic in vitro. For Styrylquinolines Perkin condensation reaction type from 8-hydroxyquinaldine with aromatic aldehydes was used. Antimalarial activity was performed using the method Radioisotope with FCB-2 strains of Plasmodium falciparum (chloroquine-resistant) and for the cytotoxic activity the MTT method with HepG2 cells was employed. Most compounds showed to be active antimalarial. Those with higher activity were Q.3 (IC₅₀ 6.4µM) and Q.5 (IC₅₀10.8 µM), although all of them were cytotoxic at concentrations above 1 µg / mL. The structures of these compounds were confirmed using infrared spectroscopy techniques and MRI in one and two dimensions.

Palabras clave : styrylquinolines; antimalarial; citotoxicity; Perkin reaction; o-alkylated compounds.

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