Fernandes P B, Shipkowitz N, Bower R R, Jarvis K P, Weisz J, Chu D T
J Antimicrob Chemother. 1986 Dec;18(6):693-701. doi: 10.1093/jac/18.6.693.
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.
双氟沙星(A-56619)、A-56620和氧氟沙星对多种厌氧菌的最低抑菌浓度(MIC)相似,或相差1至2倍稀释度。环丙沙星的活性略低于双氟沙星、A-56620和氧氟沙星(相差2至4倍稀释度)。诺氟沙星对厌氧菌的活性低于所测试的其他氟喹诺酮类药物。除革兰氏阳性球菌外,诺氟沙星、A-56620、环丙沙星和氧氟沙星在pH 8.1时对大多数厌氧菌的MIC低于pH 6.6时。氟喹诺酮类药物对厌氧球菌的MIC在pH 6.6、7.3和8.1时相同。诺氟沙星和环丙沙星受酸性pH的影响最大。与诺氟沙星和环丙沙星相比,氧氟沙星和A-56620受酸性pH的影响较小。在测试的三个pH值下,双氟沙星的效力相似。采用小鼠皮下厌氧菌感染模型来确定新型氟喹诺酮类药物对脆弱拟杆菌的体内疗效。在该试验中,双氟沙星是最有效的化合物。