Vermote Arno, Van Calenbergh Serge
Laboratory for Medicinal Chemistry, Ghent University , Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
ACS Infect Dis. 2017 Nov 10;3(11):780-796. doi: 10.1021/acsinfecdis.7b00084. Epub 2017 Oct 4.
Antimicrobial resistance constitutes a global health problem, while the discovery and development of novel antibiotics is stagnating. Methicillin-resistant Staphylococcus aureus, responsible for the establishment of recalcitrant, biofilm-related infections, is a well-known and notorious example of a highly resistant micro-organism. Since resistance development is unavoidable with conventional antibiotics that target bacterial viability, it is vital to develop alternative treatment options on top. Strategies aimed at more subtle manipulation of bacterial behavior have recently attracted attention. Here, we provide a literature overview of several small-molecule potentiators for antibiotics, identified for the treatment of Staphylococcus aureus infection. Typically, these potentiators are not bactericidal by themselves and function by reversing resistance mechanisms, by attenuating Staphylococcus aureus virulence, and/or by interfering with quorum sensing.
抗生素耐药性是一个全球性的健康问题,而新型抗生素的发现和开发却停滞不前。耐甲氧西林金黄色葡萄球菌是一种高度耐药的微生物,它会引发顽固的、与生物膜相关的感染,是一个广为人知的臭名昭著的例子。由于针对细菌生存能力的传统抗生素不可避免地会产生耐药性,因此开发其他治疗方案至关重要。旨在更巧妙地操纵细菌行为的策略最近受到了关注。在这里,我们提供了一份文献综述,介绍了几种用于治疗金黄色葡萄球菌感染的抗生素小分子增效剂。通常,这些增效剂本身不具有杀菌作用,其作用机制是逆转耐药机制、减弱金黄色葡萄球菌的毒力和/或干扰群体感应。