Potent Irreversible Inhibitors of LasR Quorum Sensing in Pseudomonas aeruginosa

ACS Medicinal Chemistry Letters
2015.0

Abstract

Antagonism of quorum sensing represents a promising new antivirulence approach for the treatment of bacterial infection. The development of a novel series of non-natural irreversible antagonists of P. aeruginosa LasR is described. The lead compounds identified (25 and 28) display potent LasR antagonist activity and inhibit expression of the P. aeruginosa virulence factors pyocyanin and biofilm formation in PAO1 and PA14.

Knowledge Graph

Similar Paper

Potent Irreversible Inhibitors of LasR Quorum Sensing in Pseudomonas aeruginosa
ACS Medicinal Chemistry Letters 2015.0
Development of a novel series of non-natural triaryl agonists and antagonists of the Pseudomonas aeruginosa LasR quorum sensing receptor
Bioorganic & Medicinal Chemistry 2017.0
Design, synthesis, and evaluation of compounds capable of reducing Pseudomonas aeruginosa virulence
European Journal of Medicinal Chemistry 2020.0
Design and synthesis of novel benzimidazole derivatives as potential Pseudomonas aeruginosa anti-biofilm agents inhibiting LasR: Evidence from comprehensive molecular dynamics simulation and in vitro investigation
European Journal of Medicinal Chemistry 2022.0
Synthetic ligands that activate and inhibit a quorum-sensing regulator in Pseudomonas aeruginosa
Bioorganic & Medicinal Chemistry Letters 2008.0
Immunosuppressive but Non-LasR-Inducing Analogues of the Pseudomonas aeruginosa Quorum-Sensing Molecule N-(3-Oxododecanoyl)-<scp>l</scp>-homoserine Lactone
Journal of Medicinal Chemistry 2011.0
Pyrogallol and its analogs can antagonize bacterial quorum sensing in Vibrio harveyi
Bioorganic &amp; Medicinal Chemistry Letters 2008.0
A comparative study of non-native N-acyl l-homoserine lactone analogs in two Pseudomonas aeruginosa quorum sensing receptors that share a common native ligand yet inversely regulate virulence
Bioorganic &amp; Medicinal Chemistry 2018.0
Anti-PqsR compounds as next-generation antibacterial agents against Pseudomonas aeruginosa: A review
European Journal of Medicinal Chemistry 2019.0
Pseudomonas aeruginosa Quorum Sensing Systems as Drug Discovery Targets: Current Position and Future Perspectives
Journal of Medicinal Chemistry 2018.0