Allicin-inspired pyridyl disulfides as antimicrobial agents for multidrug-resistant Staphylococcus aureus
作者:Jordan G. Sheppard、Jeremy P. McAleer、Pushkar Saralkar、Werner J. Geldenhuys、Timothy E. Long
DOI:10.1016/j.ejmech.2017.10.018
日期:2018.1
S-alkyl chains of 7–9 carbons in length. Further biological studies revealed that the disulfides display synergy with vancomycin against VRSA, cause dispersal of S. aureus biofilms, exhibit low cytotoxicity, and decelerate S. aureus metabolism. In final analysis, pyridyl disulfides represent a novel class of mechanism-based antibacterial agents that have a potential application as antibiotic adjuvants in
评估了由19种合成的吡啶基二硫化物组成的化学文库,这些化合物模拟了大蒜素(大蒜)的化学反应性,从而对一组病原菌具有抗菌活性。革兰氏阳性菌种(包括万古霉素中间体和耐万古霉素的金黄色葡萄球菌(VISA,VRSA))对具有7–9个碳原子的S-烷基链类似物的敏感性最高。进一步的生物学研究表明,二硫化物显示出与万古霉素抗VRSA的协同作用,引起金黄色葡萄球菌生物膜的散布,细胞毒性低,并使金黄色葡萄球菌减速。代谢。归根结底,吡啶基二硫化物代表了一类新型的基于机理的抗菌剂,它们在抗菌药物中具有潜在的应用,可在万古霉素敏感性降低的金黄色葡萄球菌感染的联合治疗中应用。