Design, Synthesis and Biological Evaluation of Benzoheterocyclic Sulfoxide Derivatives as Quorum Sensing Inhibitors in Pseudomonas Aeruginosa

SSRN Electronic Journal(2022)

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摘要
Six series of benzoheterocyclic sulfoxide derivatives were designed and synthesised as () quorum sensing inhibitors in this paper. We experimentally demonstrated that significantly inhibited the formation of PAO1 biofilm without affecting the growth. Further mechanistic studies showed that affected the luminescence of quorum sensing reported strain PAO1-- and the production of PAO1 elastase virulence factor which was regulated by system. These experimental results indicate that acts as a quorum sensing inhibitor mainly through the system. Furthermore, silico molecular docking studies demonstrated that and the quorum sensing receptor LasR were molecularly bound via hydrogen bonding interactions. Preliminary structure-activity relationship and docking studies illustrated that shows great promise as anti-biofilm compounds for further studies in order to solve the problem of microbial resistance in future.
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关键词
Pseudomonas aeruginosa,Sulfoxide,biofilm,inhibitors,quorum sensing
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