[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].
OBJECTIVE
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.


CONCLUSIONS
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.
Liu
J Y
JY
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Wei
Y G
YG
Guo
H Y
HY
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects
D000890:Anti-Infective Agents; D011725:Pyridines; D015363:Quinolones; D002939:Ciprofloxacin