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

Authors : Ayşegül Gümüş, Veysi Okumuş

Pages : 1344-1357

View : 12 | Download : 8

Publication Date : 9999-12-31

Article Type : Makaleler

Abstract :  One-pot synthesis of novel quinoline- and quinolone-substituted 1,2,3-triazoles has been performed from the key intermediates, quinoline- and quinolone-substituted propargyl derivatives 1-3 (48%-88% yields). The antioxidant properties 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 scavenging effects of compounds on the free radical decreased in the order of 3b > " role="presentation"> > > > 3a > " role="presentation"> > > > 1b } and were found to be 36.3%, 34.9%, and 27.6% at the concentration of 500 μ " role="presentation"> μ μ \mu g/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 DNA binding ability of the compounds was evaluated with calf thymus DNA using agarose gel electrophoresis.
Keywords : Quinoline, quinolone, triazole, antioxidant, antibacterial