FA103 is a newly developed quinolone derivative with a seven-membered ring, perhydrodiazepinone, at the C-7 position.
The
in vitro antibac terial activity of FA103 against a panel of bacterial type strains, including methicillin-resistant
Staphylococcus aureus strains, was compared with that of ofloxacin, nor floxacin, ciprofloxacin and sparfloxacin.
The activity of FA103 against Gram-positive bacteria and methicillin-resistant
Staphylococcus aureus, was higher than those of other quinolones, and its activity against Gram-negativ e bacteria was equal to or less than those of other quinolones. FA103 was 2 to 8 times more active than sparfloxa cin against Gram-positive bacteria including methicillin-resistant
Staphylococcus aureus, and was 2 to 8 times less active than sparfloxacin against Gram-negative bacteria so far tested.
The
in vitro antibacterial profile of FA103 is similar to that of sparflo xacin, which shows potent concentration-dependent bactericidal activity against
Staphylococcus aureus, Escherichia coli and
Pseudomonas aeruginosa. FA103 showed potent bactericidal activity and inhibited the super-coiling activity of DNA gyrase.
In addition, FA103 was more active than other quinolones against
Streptococcus pyogenes and
Streptococcus pneumoniae.
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