Abstract Two novel series of chalcone-based homoserine lactones were synthesized and their quorum sensing (QS) inhibitory activity was evaluated against Pseudomonas aeruginosa in vitro. Furthermore these compounds’ capacity for modulation of the LasR -dependent quorum sensing system of P. aeruginosa was identified. Among these compounds, ( S )-2-((4-(3-(4-bromo-2-fluorophenyl) acryloyl) phenyl) amino)- N -(2-oxotetrahydrofuran-3-yl)acetamide exerted the inhibition of LasR -dependent QS system of P. aeruginosa in contrast to brominated furanone C30 . Worthy of particular note, this research has delivered novel potent quorum sensing inhibitors (QSIs), which strongly inhibit the production of virulence factors in a wild type strain of this pathogenic bacterium.

中文翻译：

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新型查耳酮基 L-高丝氨酸内酯的合成及其群体感应抑制活性评价

摘要 合成了两个新系列的查尔酮基高丝氨酸内酯，并在体外评估了它们对铜绿假单胞菌的群体感应（QS）抑制活性。此外，还鉴定了这些化合物调节铜绿假单胞菌的 LasR 依赖性群体感应系统的能力。在这些化合物中，( S )-2-((4-(3-(4-bromo-2-fluorophenyl) acryloyl) phenyl)amino)-N -(2-oxotetrahydrofuran-3-yl)乙酰胺对LasR有抑制作用与溴化呋喃酮 C30 相比，铜绿假单胞菌的依赖 QS 系统。值得特别注意的是，这项研究提供了新型有效的群体感应抑制剂 (QSI)，它可以强烈抑制这种病原菌野生型菌株中毒力因子的产生。