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Synthesis, Molecular Docking, and Biofilm Formation Inhibitory Activity of 5‐Substituted 3,4‐Dihalo‐5 H ‐furan‐2‐one Derivatives on Pseudomonas aeruginosa
Author(s) -
Liu GuoYong,
Guo BaoQin,
Chen WanNa,
Cheng Chao,
Zhang QianLan,
Dai MiBei,
Sun JunRong,
Sun PingHua,
Chen WeiMin
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2012.01342.x
Subject(s) - biofilm , pseudomonas aeruginosa , chemistry , furan , docking (animal) , microbiology and biotechnology , aryl , minimum inhibitory concentration , antimicrobial , bacteria , stereochemistry , biology , organic chemistry , medicine , genetics , alkyl , nursing
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‐5 H ‐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‐5 H ‐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.