Design, synthesis and biological evaluation of 4-(alkyloxy)-6-methyl-2H-pyran-2-one derivatives as quorum sensing inhibitors

作者：Park Suzie; Kim Han Shin; Ok Kiwon; Kim YunHye; Park Hee Deung; Byun Youngjoo^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(15): 2913-2917.

DOI：10.1016/j.bmcl.2015.05.054

• Quorum sensing
• Biofilm inhibition
• Pyrone
• Pseudomonas aeruginosa

Novel pyrone-derived quorum sensing (QS) ligands to inhibit the binding of OdDHL to the LasR of Pseudomonas aeruginosa were designed, synthesized and evaluated. Among the analogs, the most potent compound 8 exhibited strong in vitro inhibitory activities against biofilm formation and down-regulated OdDHL/LasR-associated genes by 35-67%. The binding mode of 8 in silico was highly similar to that of the crystal ligand OdDHL in the active site of LasR.

• 出版日期2015-8-1