[In vitro and in vivo antibacterial activities of a new quinolone derivative, FD501].
FD501 is a newly synthesized quinolone derivative with aminoazepine group at the C-7 position. The in vitro and in vivo antibacterial activities of FD501 were investigated comparing with those of norfloxacin, ofloxacin, ciprofloxacin and sparfloxacin. The in vitro antibacterial activities of FD501 against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus, were equal to or higher than those of other quinolones. But its activities against Gram-negative bacteria were equal to or lower than those of other quinolones. Minimum inhibitory concentrations of FD501 against Gram-positive bacteria were similar to that of sparfloxacin. The bactericidal activity may be due to the inhibition of the DNA super-coiling activity of DNA gyrase. The area under the serum concentration-time curve of FD501 in rats following oral administration was larger than norfloxacin and ciprofloxacin and smaller than those of ofloxacin and sparfloxacin.
Imamori
K
K
United Graduate School of Agricultural Sciences of Gifu University.
Asaoka
T
T
Matsumoto
M
M
Maebashi
K
K
Matsuda
H
H
Tahara
Y
Y
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008297:Male; D008826:Microbial Sensitivity Tests; D051381:Rats; D017207:Rats, Sprague-Dawley; D059005:Topoisomerase II Inhibitors
D042462:4-Quinolones; D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; C099098:FD 501; D059005:Topoisomerase II Inhibitors; D002939:Ciprofloxacin