[Studies on pyridonecarboxylic acids as antibacterial agents.  XII. Synthesis and antibacterial activity of 6-chloro-1-cyclopropyl-7-(1-piperazinyl)-1, 4-dihydro-4-oxo-quinoline-3-carboxylic acid and analogues].
Sixteen pyridonecarboxylic acids, characterized by having a chlorine atom and a cyclopropyl group at the 6- and 1-position respectively, substituted amino groups at the 7-position, and some substituted groups (chloro, nitro, amino, dimethylamino) at the 8-position, were synthesized. In vitro antibacterial activities of these compounds were tested. The fluoroquinolones ciprofloxacin and norfloxacin were included for comparative purposes. The results showed that both 11 Ca and 11 Cc were 4-8 times more active than ciprofloxacin and norfloxacin against S. aureus-15 in vitro, but with the same activity as ciprofloxacin against E. coli-22 and P. aeruginosa-29.
Li
X H
XH
Institute of Medicinal Biotechnology, Chinese Acadeny of Medical Sciences, Peking Union Medical College, Beijing 100050.
Tian
Z M
ZM
Miao
H
H
Yu
L X
LX
Guo
H Y
HY
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D051379:Mice; D009643:Norfloxacin / Q000494:pharmacology; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology; D013203:Staphylococcal Infections / Q000188:drug therapy; D013211:Staphylococcus aureus / Q000187:drug effects
D000890:Anti-Infective Agents; D002264:Carboxylic Acids; D011728:Pyridones; D015363:Quinolones; D002939:Ciprofloxacin; D009643:Norfloxacin