Small molecule inhibitors of bacterial quorum sensing and biofilm formation
Small molecule inhibitors of bacterial quorum sensing and biofilm formation
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DOI：
10.1021/ja0530321
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发表时间：
2005-09-21
影响因子：
15
通讯作者：
Blackwell, HE
中科院分区：
文献类型：
--
作者：
Geske, GD;Wezeman, RJ;Blackwell, HE
细菌通过一种称为群体感应的小分子（或自诱导物）来监测其局部种群密度。在这里，我们报告了一种新的和有效的合成路线，天然存在的细菌自诱导剂[N-酰基高丝氨酸内酯（AHLs）]，很容易服从类似物的合成。该途径已应用于非天然AHLs文库的首次合成。这些化合物在细菌报告基因和生物膜测定的评价揭示了一组有效的群体感应拮抗剂。这些配体将作为探索群体感应在细菌致病中的作用的有价值的新工具。
Bacteria monitor their local population densities using small molecules (or autoinducers) in a process known as quorum sensing. Here, we report a new and efficient synthetic route to naturally occurring bacterial autoinducers [N-acyll-homoserine lactones (AHLs)] that is readily amenable to the synthesis of analogues. This route has been applied in the first synthesis of a library of non-native AHLs. Evaluation of these compounds in bacterial reporter gene and biofilm assays has revealed a potent set of quorum sensing antagonists. These ligands will serve as valuable new tools to explore the role of quorum sensing in bacterial pathogenesis.