Staphylococcus aureus is the pathogen responsible for the majority of human skin infections. In particular, the methicillin‐resistant variety, MRSA, has become a global clinical concern. The extensive use of mupirocin, the first‐line topical antibacterial drug of choice, has led to the emergence of mupirocin‐resistant MRSA globally, resulting in the urgent need for a replacement. Antimicrobial peptides are deemed plausible candidates. Herein, we describe a structure–activity relationship approach in the design of an ultra‐short peptide with potent anti‐MRSA activity with a rapid, bactericidal mode of action. Coupled to a low cytotoxic activity, we believe our lead compound can be developed into a topical antibacterial agent to replace mupirocin as the first‐line drug for treating MRSA skin infections.

中文翻译：

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设计具有对耐Mupirocin的MRSA的有效活性的超短抗菌肽

金黄色葡萄球菌是引起大多数人类皮肤感染的病原体。尤其是，耐甲氧西林的品种MRSA已成为全球临床关注的问题。首选的一线局部抗菌药物莫匹罗星的广泛使用已导致耐莫匹罗星的MRSA在全球范围内出现，因此迫切需要替代药物。抗菌肽被认为是可能的候选物。在本文中，我们描述了一种结构-活性关系方法，该方法设计具有有效的抗MRSA活性并具有快速杀菌作用的超短肽。加上较低的细胞毒活性，我们认为我们的先导化合物可以发展成为局部抗菌剂，以代替莫匹罗星作为治疗MRSA皮肤感染的一线药物。