Results
Title

Síntesis de estirilquinolinas con potencial Leishmanicida in vitro sobre Leishmania (Viannia) panamensis.

Authors

Torres, Omar L.; Marin, Fernis J.; Santafé, Gilmar G.; Robledo, Sara M.

Abstract

A Perkin type condensation reaction between quinaldine and 8-hydroxyquinaldine with aromatic aldehydes, three styrylquinolines were synthesized: (E)-2-ethoxy-4-(2-(8-hydroxyquinolin-2-il)vinyl)phenyl acetate (1), 2- [(E)-2-(2-acetiloxy-5-nitrophenyl)ethenyl] quinoline (2), 2-[(E)-2-(3-methoxyiphenyl)ethenyl] quinoline (3). The leishmanicidal potential in vitro employing flow cytometry was determined and the cytotoxicity by MTT method, was evaluated. The compounds (1) y (2) showed to be active against Leishmania (V) panamensis with lethal dose 50%) (LD50) de 0.2 and 2.5 μg/mL, LD50 de 2.8 and 5.9 μg/mL and selectivity index of 14.0 and 2.4, respectively, compared to the drug control amphotericin B. The structures of these compounds were confirmed using spectroscopic techniques from analysis: IR, ¹H and 13C NMR, COSY, HMQC, HMBC and DEPT experiments. Three styrylquinolines were synthesized with performance of 40.3%, 72.0% and 80.0% respectively, styrylquinolines (1) and (2) showed good leishmanicidal potential with inhibition percentages of 67.5 y 74.9 respectively.

Subjects

PHENYLACETATES; CONDENSATION reactions; DRUG control; FLOW cytometry; LEISHMANIA; AROMATIC aldehydes

Publication

Información Tecnológica, 2020, Vol 31, Issue 1, p3

ISSN

0716-8756

Publication type

Academic Journal

DOI

10.4067/S0718-07642020000100003