Synthesis, pharmacokinetics, and biological activity of a series of new pyridonecarboxylic acid antibacterial agents bearing a 5-fluoro-2-pyridyl group or a 3-fluoro-4-pyridyl group at N-1

The 1‐(5‐fluoro‐2‐pyridyl) or 1‐(3‐fluoro‐4‐pyridyl) group was introduced in the syntheses of new pyridonecarboxylic acid antibacterial agents. 1‐(5‐Fluoro‐2‐pyridyl)‐6‐fluoro‐1,4‐dihydro‐7‐(4‐methyl‐1‐piperazinyl)‐4‐oxoquinolone‐3‐carboxylic acid 7b (DW‐116) showed a moderate in vitro antibacterial activity but it was found to have very excellent pharmacokinetic profiles so that 7b (DW‐116) showed dramatic increased in vivo efficacy.