Journal of Medicinal Chemistry p. 2163 - 2169 (1987)
Update date:2022-08-02
Topics:
Uno, Toshio
Takamatsu, Masanori
Inoue, Yoshimasa
Kawahata, Yoshihiro
Iuchi, Koji
Tsukamoto, Goro
A series of 6-fluoro- and 6,8-difluoro-7-(azole substituted)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids were prepared.Structure-activity relationship studies indicated that the antibacterial potency was better when the 6,8-substituents were fluorine atoms and the 7-substituent was either 1-imidazolyl, 20, or 4-methyl-1-imidazolyl, 25.From the results of studies on pharmacokinetic profile and toxicity, 20 and 25 were found to possess excellent antibacterial activities and to show high blood levels after oral administration to mice with low toxicity.
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