Design, synthesis and antibacterial activity of fluoroquinolones containing bulky arenesulfonyl fragment: 2D-QSAR and docking study

► Arenesulfonylquinolones were synthesized and evaluated for antibacterial activity. ► Most compounds exhibited significant antibacterial activity. ► Antibacterial activity depends on the electronic effect of substituent groups. ► 2D-QSAR models provide fine relationship linking structure and activity. ►Docking study of the most active 3b revealed similar binding mode to ciprofloxacin.