A DNA gyrase inhibitor
Sparfloxacin (CI-978) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity.
Sparfloxacin (CI-978) shows broad and potent antibacterial activity. Its MICs for 90% of the strains tested are 0.1 to 0.78 μg/ml against gram-positive organisms, such as members of the genera Staphylococcus , Streptococcus and Enterococcus , and 0.0125 to 1.56 μg/ml against gram-negative organisms, such as members of the family Enterobacteriaceae and the genera Pseudomona . Its MICs are 0.025 to 0.78 μg/ml against glucose nonfermenters, 0.2 to 0.78 μg/ml against anaerobes, 0.0125 to 0.05 μg/ml against Legionella. Sparfloxacin (CI-978) showed good oral efficacy against systemic infections with Staphylococcus aureus , Streptococcus pyogenes , Streptococcus pneumoniae , Escherichia coli , and Pseudomonas aeruginosa in mice[1]. Sparfloxacin targets DNA gyrase and inhibits DNA synthesis[2].
参考文献:
[1]. Nakamura, S., et al., In vitro and in vivo antibacterial activities of AT-4140, a new broad-spectrum quinolone. Antimicrob Agents Chemother, 1989. 33(8): p. 1167-73.
[2]. Pan, X.S. and L.M. Fisher, Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones. Antimicrob Agents Chemother, 1997. 41(2): p. 471-4.
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