（S）-（-）-9-氟-2,3-二氢-3-甲基-10-[4-（2-吡啶基）-1-哌嗪基]-7-氧代-7H-吡啶并[1,2,3-de][1,4]苯并恶嗪-6-羧酸（YH-6）与其他抗生素相比的体外抗支原体活性

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.

作者信息

Ye H, Wu J M, Yang Y S, Ji R Y, Chen K X

机构信息

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 200032, China.

出版信息

Zhongguo Yao Li Xue Bao. 1999 Nov;20(11):1031-4.

PMID:11270970

Abstract

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 micrograms.L-1), Mycoplasma hominis (Mh: 500 micrograms.L-1), M orale (Mo: 125 micrograms.L-1) and M salivarium (Ms: 125 micrograms.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. EMr- or Tcr- strains of Uu (or Mh) had no cross-resistance to YH-6.

摘要

目的

测定支原体和脲原体对（S）-（-）-9-氟-2,3-二氢-3-甲基-10-[4-（2-吡啶基）-1-哌嗪基]-7-氧代-7H-吡啶并[1,2,3-de][1,4]苯并恶嗪-6-羧酸（YH-6）的敏感性，并与参考喹诺酮类、大环内酯类和四环素类药物进行比较。

方法

采用微量稀释法体外测定最低抑菌浓度（MIC）。

结果

YH-6对解脲脲原体（Uu：250微克/升）、人型支原体（Mh：500微克/升）、口腔支原体（Mo：125微克/升）和唾液支原体（Ms：125微克/升）的MIC与大环内酯类药物（红霉素和柱晶白霉素）相近，比氧氟沙星（Ofl）高2-8倍。Uu和Mh易对红霉素和四环素产生耐药性。它们不易对喹诺酮类（YH-6、Ofl）、交沙霉素和泰乐菌素产生耐药性。Uu（或Mh）的四环素耐药（Tcr）或红霉素耐药（EMr）菌株对红霉素或四环素存在交叉耐药性。然而，它们对喹诺酮类、交沙霉素和泰乐菌素没有交叉耐药性。