<I>IN VITRO</I> AND <I>IN VIVO</I> ANTIBACTERIAL ACTIVITIES OF A NEW QUINOLONE DERIVATIVE, FD501

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  • 新規キノロン系化合物, FD501の <I>in vitro</I> および <I>in vivo</I> 抗菌活性

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Abstract

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.<BR>The in vitro antibacterial activities of FD501 against Gram-positive bacteria including methicillinresistant 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.<BR>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 supercoiling activity of DNA gyrase.<BR>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 sparnoxacin.

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