4.6 Article

Design, synthesis and evaluation of halogenated furanone derivatives as quorum sensing inhibitors in Pseudomonas aeruginosa

期刊

出版社

ELSEVIER
DOI: 10.1016/j.ejps.2019.105058

关键词

Furanones; Quorum sensing; Pseudomonas aeruginosa; Biofilm

资金

  1. National Natural Science Foundation of China [81573294, 81773593, 81872759]
  2. Excellent Young Teachers Program of Guangdong Provincial colleges and universities [YQ 2015061]
  3. Major Project for the Innovation of Industry and Research of Guangzhou City [201508020128]
  4. Pearl River S&T Nova Program of Guangzhou [201610010100]
  5. Fundamental Research Funds for the Central Universities [21617478]

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The biofilm formation of Pseudomonas aeruginosa (P. aeruginosa) is regulated by a phenomenon of quorum sensing (QS). With 5-hydroxyl-3,4-halogenated-5H-furan-2-ones as beginning, analogs bearing alkyl chains, vinyl bromide, or aromatic rings were designed and synthesized. The minimum inhibitory concentration (MIC) of the compounds against P. aeruginosa was assayed and the biofilm inhibition ratio was determined at different concentrations lower than the MIC. C-5 aromatic substituted furanones showed remarkable biofilm formation as well as inhibition of virulence factor production in P. aeruginosa. Fluorescence report analysis identified the QS regulatory mechanism of the most active compound 29. This study provides us a novel candidate for combating drug resistant bacteria strains by merely inhibiting biofilm formation. Without suppressing the regular life cycle of the bacteria, bacterial resistance mechanisms may not be activated.

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