首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >In vitro activity of the new difluorinated quinolone sparfloxacin (AT-4140) against Mycobacterium tuberculosis compared with activities of ofloxacin and ciprofloxacin.
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In vitro activity of the new difluorinated quinolone sparfloxacin (AT-4140) against Mycobacterium tuberculosis compared with activities of ofloxacin and ciprofloxacin.

机译:与氧氟沙星和环丙沙星的活性相比新型二氟喹诺酮司帕沙星(AT-4140)的体外抗结核分枝杆菌活性。

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摘要

MICs of the new fluoroquinolone drugs ofloxacin, ciprofloxacin, and sparfloxacin (AT-4140) for 10 strains of Mycobacterium tuberculosis were determined by using both a BACTEC radiometric method and testing on solid 7H11 agar medium. Radiometric MICs by 7H12 broth testing ranged from 0.5 to 1.0, 0.25 to 0.5, and 0.1 to 0.2 microgram/ml for ofloxacin, ciprofloxacin, and sparfloxacin respectively, whereas MICs in solid medium ranged from 0.5 to 1.0, 0.5 to 1.0, and 0.2 to 0.5 microgram/ml, respectively. The bactericidal action of the quinolones compared with their reported peak concentrations in human serum showed that sparfloxacin is the most bactericidal, followed by ciprofloxacin and ofloxacin. Our results suggest the potential of the new difluorinated quinolone sparfloxacin for use against the tubercle bacillus and indicate that further determination of its antimycobacterial spectrum and intracellular efficacy may be fruitful.
机译:通过使用BACTEC辐射测定法并在7H11琼脂固体培养基上进行测试,确定了10株结核分枝杆菌新氟喹诺酮药物氧氟沙星,环丙沙星和司帕沙星(AT-4140)的MIC。通过7H12肉汤测试测得的氧氟沙星的MIC范围分别为氧氟沙星,环丙沙星和司帕沙星的0.5-1.0、0.25-0.5和0.1-0.2微克/毫升,而固体培养基中的MIC范围为0.5-1.0、0.5-1.0和0.2-0.5微克/毫升。分别为0.5微克/毫升。喹诺酮类药物的杀菌作用与其在人血清中的峰值浓度相比表明,司帕沙星是最具杀菌力的,其次是环丙沙星和氧氟沙星。我们的结果表明,新型的二氟喹诺酮司帕沙星具有抗结核杆菌的潜力,并表明进一步确定其抗分枝杆菌谱和细胞内功效可能是富有成果的。

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