合成化学療法剤NM441の<I>in vitro</I>および<I>in vivo</I>抗菌力

DOI 被引用文献3件 参考文献10件

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  • <I>In vitro</I>and<I>in vivo</I>antibacterial activity of NM441

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NM441 is a prodrug of a 6-fluoroquinolone antibacterial agent. When NM441 was administered orally, it was readily absorbed and metabolized to its active form, NM394. Thein vitroandin vivoantibacterial activities of NM441 were compared with those of ofloxacin (OFLX), ciprofloxacin (CPFX), enoxacin (ENX) and tosufloxacin (TFLX). NM394 had a broad antimicrobial spectrum against gram-positive and gram-negative bacteria. The antibacterial activity of NM394 against clinical isolates of gram-positive and gram-negative bacteria was equal to or one-half that of CPFX. NM394 was as active as OFLX against gram-positive bacteria, and was 2 to 8 times more active against gram-negative bacteria, includingPseudomonas aeruginosa. The activity of NM394 was not influenced by the type of medium, inoculum size or addition of serum. The MICs of NM394 againstEscherichia coliandP. aeruginosaat pH 5.5 were reduced 4 to 16 times in comparison with those at pH7.0. The bactericidal activity of NM394 againstStaphylococcus aureus, E. coli, Serratia marcescensandP. aeruginosawas superior to those of CPFX, OFLX and TFLX. NM394 was accumulated to higher concentrations than OFLX and CPFX inS. aureus, E. coliandP. aeruginosa. In the morphological examination by the phase-contrast microscope, NM394 induced the formation of filamentous cell and lysis ofE. coliandS. marcescens, and induced the formation of spherical cell and lysis ofP. aeruginosa. The protective effect of NM441 against systemic infection caused by gram-positive and gram-negative organism in mice was superior to those of CPFX, OFLX and ENX.

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