The increase in the prevalence of antibiotic-resistant pathogens leads to a decrease in the number of antimicrobial agents for the treatment of infections and prompts researchers to search for new effective antimicrobial drugs. This study reports the synthesis of novel triphenylphosphonium-functionalized substituted pyrimidines and in vitro evaluation of their antibacterial and antibiofilm activity. Most of the synthesized derivatives showed high antibacterial activity (MIC = 0.39–1.56 μg/mL) against the methicillin-resistant strain of S. aureus 222. Compounds 2a and 11 exhibited a high level of antibiofilm activity against S. aureus 222 and E. coli 311. The triphenylphosphonium-containing pyrimidines 11 and 2a reduced S. aureus 222 biofilm formation by 99.1% and 95.8%, respectively. In addition, compound 2a was the most active against E. coli 311 biofilm formation (the biomass decreased by 98.4%).

中文翻译：

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新型三苯基鏻功能化取代嘧啶的合成及体外抗菌和抗生物膜活性评价

抗生素耐药病原体流行率的增加导致用于治疗感染的抗菌药物数量减少，并促使研究人员寻找新的有效抗菌药物。本研究报道了新型三苯基鏻功能化取代嘧啶的合成及其抗菌和抗生物膜活性的体外评价。大多数合成的衍生物对金黄色葡萄球菌222 的甲氧西林耐药菌株表现出高抗菌活性（MIC = 0.39–1.56 μg/mL）。化合物2a和11对金黄色葡萄球菌222 和大肠杆菌表现出高水平的抗生物膜活性。大肠杆菌311。含三苯基鏻的嘧啶11和2a分别使金黄色葡萄球菌222 生物膜形成减少99.1% 和 95.8%。此外，化合物2a对大肠杆菌311 生物膜形成最具活性（生物量减少了 98.4%）。