Synthesis and biological evaluation of quinoline-triazole and quinolone-triazole conjugates

Abstract

One-pot synthesis of novel quinoline- and quinolone-substituted 1,2,3-triazoles has been performed from thekey intermediates, quinoline- and quinolone-substituted propargyl derivatives 1–3 (48%–88% yields). The antioxidantproperties of the newly synthesized compounds, 1a–1c, 2a–2c, and 3a–3c, were evaluated by monitoring DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging abilities, metal chelating effects, and reducing power. The scavengingeffects of compounds on the free radical decreased in the order of 3b > 3a > 1b and were found to be 36.3%, 34.9%,and 27.6% at the concentration of 500 µg/mL, respectively. All of the compounds showed low chelating capacity.Furthermore, the antibacterial activity was studied against gram-positive and gram-negative bacteria and the DNAbinding ability of the compounds was evaluated with calf thymus DNA using agarose gel electrophoresis.