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新型喹诺酮类药物PD127,391的体外活性

The in-vitro activity of PD127,391, a new quinolone.

作者信息

King A, Boothman C, Phillips I

机构信息

Department of Microbiology, UMDS, London, UK.

出版信息

J Antimicrob Chemother. 1988 Aug;22(2):135-41. doi: 10.1093/jac/22.2.135.

Abstract

MICs of PD127,391 a new 4-quinolone, and of CI934 and ciprofloxacin, two previously reported 4-quinolones, were determined for common clinical bacterial isolates by an agar-dilution method. PD127,391 was the most active drug against Enterobacteriaceae and Acinetobacter spp (MICs less than 0.12 mg/l) and as active as ciprofloxacin against Aeromonas spp. (MICs less than 0.008 mg/l) and Pseudomonas aeruginosa (MICs less than 1 mg/l). It was more active than ciprofloxacin against Pseudomonas spp. including Ps. maltophilia (MICs less than 0.25 mg/l). All three drugs had high activity, with PD129,391 again the best, against Haemophilus influenzae Brahmamella catarrhalis, and Neisseria gonorrhoeae. PD127,391 was much more active than the other drugs against Campylobacter coli/jejuni (PD127,391 MICs less than 0.03 mg/l) and Gardnerella vaginalis (PD127,391 MICs less than 0.25 mg/l). PD127,391 inhibited all staphylococci at less than 0.06 mg/l and streptococci at less than 0.5 mg/l, thus being more active than CI934 or ciprofloxacin. PD127,391 was much more active against anaerobic cocci, Bacteroides spp. and clostridia (including Clostridium difficile) (MICs less than 1 mg/l) than was CI934 (MICs less than 16 mg/l) or ciprofloxacin (MICs less than 64 mg/l). No bacterium that we examined required more than 1 mg/l of PD127,391 for inhibition, and there was no cross resistance with unrelated antibiotics.

摘要

采用琼脂稀释法测定了新型4-喹诺酮类药物PD127391以及两种先前报道的4-喹诺酮类药物CI934和环丙沙星对常见临床分离细菌的最低抑菌浓度(MIC)。PD127391是对肠杆菌科细菌和不动杆菌属最具活性的药物(MIC小于0.12mg/L),对气单胞菌属(MIC小于0.008mg/L)和铜绿假单胞菌(MIC小于1mg/L)的活性与环丙沙星相当。它对包括嗜麦芽窄食单胞菌在内的假单胞菌属的活性比环丙沙星更高(MIC小于0.25mg/L)。这三种药物对流感嗜血杆菌、卡他莫拉菌和淋病奈瑟菌均具有高活性,其中PD129391的活性最佳。PD127391对大肠弯曲菌/空肠弯曲菌(PD127391的MIC小于0.03mg/L)和阴道加德纳菌(PD127391的MIC小于0.25mg/L)的活性远高于其他药物。PD127391对所有葡萄球菌的抑菌浓度小于0.06mg/L,对链球菌的抑菌浓度小于0.5mg/L,因此比CI934或环丙沙星更具活性。PD127391对厌氧球菌、拟杆菌属和梭菌(包括艰难梭菌)的活性(MIC小于1mg/L)远高于CI934(MIC小于16mg/L)或环丙沙星(MIC小于64mg/L)。我们检测的细菌中没有一种需要超过1mg/L的PD127391来抑制,并且与不相关抗生素不存在交叉耐药性。

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