新型利福霉素对耐利福霉素金黄色葡萄球菌的体外活性
In vitro activity of novel rifamycins against rifamycin-resistant Staphylococcus aureus.
作者信息
Murphy Christopher K, Mullin Steve, Osburne Marcia S, van Duzer John, Siedlecki Jim, Yu Xiang, Kerstein Kathy, Cynamon Michael, Rothstein David M
机构信息
ActivBiotics, Inc., 110 Hartwell Avenue, Lexington, Massachusetts 02421, USA.
出版信息
Antimicrob Agents Chemother. 2006 Mar;50(3):827-34. doi: 10.1128/AAC.50.3.827-834.2006.
Abstract
We describe novel rifamycin derivatives (new chemical entities [NCEs]) that retain significant activity against a comprehensive collection of Staphylococcus aureus strains that are resistant to rifamycins. This collection of resistant strains contains 21 of the 26 known single-amino-acid alterations in RpoB, the target of rifamycins. Some NCEs also demonstrated a lower frequency of resistance development than rifampin and rifalazil in S. aureus as measured in a resistance emergence test. When assayed for activity against the strongest rifamycin-resistant mutants, several NCEs had MICs of 2 microg/ml, in contrast to MICs of rifampin and rifalazil, which were 512 microg/ml for the same strains. The properties of these NCEs therefore demonstrate a significant improvement over those of earlier rifamycins, which have been limited primarily to combination therapy due to resistance development, and suggest a potential use of these NCEs for monotherapy in several clinical indications.
摘要
我们描述了新型利福霉素衍生物（新化学实体[NCEs]），它们对一系列对利福霉素耐药的金黄色葡萄球菌菌株仍具有显著活性。这组耐药菌株包含利福霉素靶点RpoB中26种已知单氨基酸改变中的21种。在耐药性出现试验中检测发现，一些NCEs在金黄色葡萄球菌中产生耐药性的频率也比利福平及利福拉齐低。在针对最强的利福霉素耐药突变体进行活性检测时，几种NCEs的最低抑菌浓度（MIC）为2微克/毫升，相比之下，相同菌株的利福平和利福拉齐的MIC为512微克/毫升。因此，这些NCEs的特性表明，与早期利福霉素相比有显著改进，早期利福霉素主要因耐药性发展而限于联合治疗，这些NCEs显示出在几种临床适应症中用于单药治疗的潜在用途。
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