Evaluation of antimalarial and cytotoxic activity of styrylquinolines obtained from 8-hydroxyquinaldine with aromatic aldehydes

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 (IC50 10.8 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. © 2014, Centro de Informacion Tecnologica. All rigths reserved.