Potent small-molecule suppression of oxacillin resistance in methicillin-resistant Staphylococcus aureus.

Potent small-molecule suppression of oxacillin resistance in methicillin-resistant Staphylococcus aureus.
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DOI:
10.1002/anie.201206911
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发表时间:
2012-11-05
影响因子:
16.6
通讯作者:
Melander, Christian
Melander, Christian
中科院分区:
化学1区
文献类型:
--
作者:
Harris, Tyler L.;Worthington, Roberta J.;Melander, Christian

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使用能够恢复多重耐药细菌(如MRSA)对临床可用抗生素的敏感性的佐剂分子是开发新型抗微生物剂的有希望的替代方案。我们报告了一种非常有效的小分子,在亚MIC水平下,可将苯唑西林对许多MRSA菌株的MIC降低高达512倍。初步的机理研究表明,VraSR双组分系统在该化合物的活性中起作用。
The use of adjuvant molecules that have the ability to restore the susceptibility of multi-drug resistant bacteria, such as MRSA, to clinically available antibiotics is a promising alternative to the development of novel antimicrobials. We report an extremely potent small molecule that, at sub-MIC levels, lowers the MIC of oxacillin against a number of MRSA strains by up to 512-fold. Preliminary mechanistic investigations indicate that the VraSR two-component system plays a role in the activity of this compound.
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