Abstract:
Eighteen pyridonecarboxylic acids, characterized by a methyl group at the C
6-position instead of the usual florine atom, cyclopropyl at the N
1-position, substituted amino groups at the C
7-position, and some subtituted groups (hydrogen, chlorine, nitro and amino) at the C
8-position, were synthesized. The
in vitro antibacterial activity of these compounds were tested, and the structure-activity relationships were also discussed. The results of the study showed that the activity of compounds 22 and 24 were less potent than that of ciprofloxacin against
S.aureus, S.epidermidis, E.coli and
P.aeruginosa, while they were 2~100 times more potent than ciprofloxacin against
K.pneumoniae, S.marcescens, A.calcoacetous, E.aerogenes, S.typhi and
S.typhimurium.