N-alkylimidazole derivatives as potential inhibitors of quorum sensing in Pseudomonas aeruginosa .

Autor: Mensah CN; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Ampomah GB; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Mensah JO; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Gasu EN; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.; Central Laboratory, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Aboagye CI; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Ekuadzi E; Central Laboratory, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.; Department of Pharmacognosy, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Boadi NO; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana., Borquaye LS; Department of Chemistry, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.; Central Laboratory, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.
Jazyk: angličtina
Zdroj: Heliyon [Heliyon] 2022 Dec 25; Vol. 8 (12), pp. e12581. Date of Electronic Publication: 2022 Dec 25 (Print Publication: 2022).
DOI: 10.1016/j.heliyon.2022.e12581
Abstrakt: Antimicrobial resistance is a threat to global public health. Microbial resistance is mediated by biofilm formation and virulence behavior during infection. Quorum sensing (QS), a cell-to-cell communication is frequently used by microbes to evade host immune systems. Inhibiting QS channels is a potential route to halt microbial activities and eliminate them. Imidazole has been shown to be a potent warhead in various antimicrobial agents. This study aims to evaluate alkyl-imidazole derivatives as potential inhibitors of QS and to explore the interactions of the compounds with LasR, a key protein in the QS machinery of Pseudomonas aeruginosa . The study revealed that imidazole derivatives with longer alkyl chains possessed better antimicrobial activities. Octylimidazole and decylimidazole emerged as compounds with better anti-virulence and biofilm inhibition properties while hexylimidazole showed the best inhibitory activity against Pseudomonas aeruginosa PAO1. The binding affinity of the compounds with LasR followed a similar trend as that observed in the QS inhibitory assays, suggesting that interaction with LasR may be important for QS inhibition.
Competing Interests: The authors declare no competing interests.
(© 2022 The Author(s).)
Databáze: MEDLINE