Synthesis, Molecular Docking, and Biofilm Formation Inhibitory Activity of 5‐Substituted 3,4‐Dihalo‐5H‐furan‐2‐one Derivatives on Pseudomonas aeruginosa
Synthesis, Molecular Docking, and Biofilm Formation Inhibitory Activity of 5‐Substituted 3,4‐Dihalo‐5H‐furan‐2‐one Derivatives on Pseudomonas aeruginosa
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DOI：
10.1111/j.1747-0285.2012.01342.x
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发表时间：
2012-05
影响因子：
3
通讯作者：
Guowei Liu;Bao-Qin Guo;Wan-Na Chen;Chao Cheng;Qian‐Lan Zhang;Mibei Dai;Jun-Rong Sun;Ping-Hua Sun;Wei-Min Chen
中科院分区：
文献类型：
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作者：
Guowei Liu;Bao-Qin Guo;Wan-Na Chen;Chao Cheng;Qian‐Lan Zhang;Mibei Dai;Jun-Rong Sun;Ping-Hua Sun;Wei-Min Chen
Pseudomonas aeruginosa (P. aeruginosa) colonize on most wounds and live as biofilm, which causes antibiotic resistance and wounds unhealed. To investigate the effects of 5‐substituted 3,4‐dihalo‐5H‐furan‐2‐one compounds on biofilm formation of P. aeruginosa, a set of 5‐(aryl‐1′‐hydroxy‐methyl)‐ or 5‐(aryl‐2‐methylene)‐3,4‐dihalo‐5H‐furan‐2‐one compounds were designed and synthesized. Their inhibitory activities on biofilm formation of P. aeruginosa were studied by MIC assay, quantitative analysis of biofilm inhibition, and observation of biofilm formation with SEM. It was found that compounds 2i, 3f, 3i showed remarkable effects of biofilm formation inhibition on P. aeruginosa. Furthermore, molecular docking was performed to identify the key structural features of these compounds with the binding site of LasR receptor.
