In-vitro and in-vivo potency of five new fluoroquinolones against anaerobic bacteria.
The MICs of difloxacin (A-56619), A-56620 and ofloxacin were similar or within one to two-fold dilutions against a variety of anaerobic bacteria. Ciprofloxacin was slightly less active (two- to four-fold dilutions) than difloxacin, A-56620 and ofloxacin. Norfloxacin was less active than the other fluoroquinolones tested against anaerobic bacteria. The MICs of norfloxacin, A-56620, ciprofloxacin and ofloxacin against most anaerobes, except the Gram-positive cocci, were lower at pH 8.1 than at pH 6.6. MICs of the fluoroquinolones against anaerobic cocci were the same at pH 6.6, 7.3 and 8.1. Norfloxacin and ciprofloxacin were most affected by the acidic pH. Ofloxacin and A-56620 were affected to a lesser extent by an acidic pH than norfloxacin and ciprofloxacin. The potency of difloxacin was similar at the three pHs tested. A subcutaneous anaerobic infection model in mice was used to determine the in-vivo efficacy of the new fluoroquinolones against Bacteroides fragilis. Difloxacin was the most potent compound in this test.
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001407:Bacillus / Q000187:drug effects; D001421:Bacteria, Anaerobic / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy; D006845:Hydrocarbons, Fluorinated / Q000494:pharmacology* / Q000627:therapeutic use; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D011809:Quinones / Q000494:pharmacology* / Q000627:therapeutic use
D000900:Anti-Bacterial Agents; D006845:Hydrocarbons, Fluorinated; D011809:Quinones