SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 5-AMINO-6, 8-DIFLUORO-1-(5-FLUORO-2-PYRIDYL)-7-(3-METHYL-1-PIPERAZINYL)-1,4-DIHYDRO-4-OXO-3-QUINOLINECARBOXYLIC ACID AND ITS ANALOGUES

AIM To design and synthesize 1-(5-fluoro-2-pyridyl) quinolone derivatives, and to study their in vitro antibacterial activities. METHODS Eight new compounds of 5-amino-6,8-difluoro-1-(5-fluoro-2-pyridyl)-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid and its analogues were synthesized from ethyl 6-nitro-2,3,4,5-terafluorobenzoylacetate and ethyl 3-methoxy 2,4,5-trifluorobenzoylacetate through 5 or 6 steps. RESULTS Fifteen new compounds (1-15) were obtained including 8 desired compounds (8-15). The structures of the compounds were determined by ¹HNMR, MS. CONCLUSION In vitro antibacterial activities of the compounds (8-15) against Staphylococcus aureus-16, Escherichia coli-26 and Pseudomonas aeruginosa-17 were lower than control of ciprofloxacin.