(S)-(-)-9-氟-2,3-二氢-3-甲基-10-[4-(2-吡啶)-1-基哌嗪]-7-氧代-7H-吡啶[1,2,3-de][1,4]苯并噁嗪-6-羧酸(YH-6)与其它抗微生物药体外抗支原体活性的比较(英文)

Antimycoplasmal activities of (S)-(-)-9-fluoro-2,3-dihydro-3-methyl-10-[4-(2-pyridyl)-1-piperazinyl ]-7-oxo-7H-pyrido [1,2,3-de] [1,4] benzoxazine-6-carboxylic acid (YH-6) in comparison with other antibiotics in vitro

目的:测定新喹诺酮YH-6对支原体的抑制活性并与其它抗微生物药剂作比较。方法:MIC的测定采用微量稀释法。结果:YH-6对解脲支原体(Uu),人型支原体(Mh),口腔支原体(Mo),唾液支原体(Ms)的MIC分别为250μg·L^(-1),500μg·L^(-1),125μg·L^(-1),125μg·L^(-1),它的抑制活性与红霉素,柱晶白霉素相当,是氧氟沙星的2-8倍。Uu,Mh对YH-6及交沙霉素和泰洛星不易产生诱导耐药性,而对红霉素和四环素易产生诱导耐药性和多重耐药性,而对YH-6,交沙霉素和泰洛星无多重耐药性。结论:YH-6对支原体有很强的抑制活性,且不易形成诱导耐药性。Uu和Mh的红霉素或四环素抗性菌株对YH-6无多重耐药性。

AIM: To determine the susceptibilities of Mycoplasma and Ureaplasma to (S)-( - )-9-fluoro-2,3-dihydro-3-methyl-10-[ 4-( 2-pyridyl )-1-piperazinyl ]-7-oxo-7H-pyrido[ 1,2,3-de ] [ 1,4 ] benzoxazine-6-carboxylic acid (YH-6) and to compare it with those referential quinolones, macrolides, and tetracyclines. METHODS: The minimum inhibitory concentration (MIC) were determined by microdilution method in vitro. RESULTS: The MIC of YH-6 for Ureaplasma urealyticum ( Uu : 250 μg· L-1), Mycoplasma hominis (Mh: 500 μg·L-1), Morale (Mo: 125 μg·L-1) and M salivarium (Ms: 125 μg·L-1) were closely similar to those of macrolides (erythromycin and leucomycin) and were 2-8 folds greater than those of ofloxacin (Ofl). Uu and Mh easily induced resistance to erythromycin and tetracycline. They did not easily form resistance to quinolone (YH-6, Ofl), josamycin and tylosin. Tetracycline-resistance (Tcr) or erythromycin-resistance (EMr) strains of Uu (or Mh) had cross-resistance to erythromycin or tetracycline. However, they had no cross-resistance to quinolone, josamycin and tylosin. CONCLUSION: YH-6 was a highly active quinolone against Mycoplasma, but could hardly induce resistance to Uu. EM- or Tcr- strainsof Uu (or Mh) had no cross-resistance to YH-6.