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.