Methicillin-resistant Staphylococcus aureus (MRSA) are challenging pathogenic bacteria that can cause severe infection leading to high mortality rates. We found that both the oxacillin- and cefoxitin-resistant S. aureus strains isolated from clinic showed multidrug-resistant (MDR) characteristics. Through rapid high-throughput screen (HTS) of a compound library, gemcitabine and selen compounds were found to effectively inhibit S. aureus growth. For further improvement, we synthesized selen-containing gemcitabine that demonstrated relatively potent antimicrobial activity against several MDR MRSA in vitro. The HTS assay and gemcitabine selen derivative provided a useful tool to explore an effective molecular target to treat MDR MRSA.

中文翻译：

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快速高通量测定确定吉西他滨及其衍生物是多药耐药金黄色葡萄球菌的有效抑制剂

耐甲氧西林金黄色葡萄球菌 (MRSA) 是具有挑战性的致病菌，可引起严重感染，导致高死亡率。我们发现从临床分离的苯唑西林和头孢西丁耐药金黄色葡萄球菌菌株均表现出耐多药（MDR）特征。通过化合物库的快速高通量筛选 (HTS)，发现吉西他滨和硒化合物可有效抑制金黄色葡萄球菌的生长。为了进一步改进，我们合成了含硒的吉西他滨，它在体外对几种 MDR MRSA 表现出相对有效的抗菌活性。HTS 测定和吉西他滨硒衍生物为探索治疗 MDR MRSA 的有效分子靶点提供了有用的工具。