Potent irreversible inhibitors of LasR quorum sensing in Pseudomonas aeruginosa

Kevin T. O'Brien; Joseph G. Noto; Luke Nichols-O'Neill; Lark J. Perez

doi:10.1021/ml500459f

Potent irreversible inhibitors of LasR quorum sensing in Pseudomonas aeruginosa

Kevin T. O'Brien, Joseph G. Noto, Luke Nichols-O'Neill, Lark J. Perez

Chemistry

Research output: Contribution to journal › Article › peer-review

56 Scopus citations

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.

Original language	English (US)
Pages (from-to)	162-167
Number of pages	6
Journal	ACS Medicinal Chemistry Letters
Volume	6
Issue number	2
DOIs	https://doi.org/10.1021/ml500459f
State	Published - Feb 12 2015

All Science Journal Classification (ASJC) codes

Biochemistry
Drug Discovery
Organic Chemistry

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10.1021/ml500459f

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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.",

author = "O'Brien, {Kevin T.} and Noto, {Joseph G.} and Luke Nichols-O'Neill and Perez, {Lark J.}",

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Y1 - 2015/2/12

N2 - 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.

AB - 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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Potent irreversible inhibitors of LasR quorum sensing in Pseudomonas aeruginosa

Abstract

All Science Journal Classification (ASJC) codes

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