ACS Medicinal Chemistry Letters · 2014 · 62 citations · 25 references
Life SciencesMedicinal ChemistryMicrobiologyAntimicrobial PharmacologyAntimicrobial PharmacotherapyAntimicrobial ResistanceAntibacterial PharmacologyAntibacterial TherapyBacterial BiofilmsBiofilm Formation In InfectionQuorum SensingQuorum Sensing In PathogenesisAnti-biofilm StrategiesBiofilm InhibitorsIrreversible InhibitionNovel Antibacterial Drug DiscoveryPseudomonas Aeruginosa Infection TreatmentQuorum Sensing InhibitionQuorum Sensing InhibitorsQuorum Sensing Receptors
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.
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