Synthetic quinolone signal analogues inhibiting the virulence factor elastase of Pseudomonas aeruginosa

We explore the chemical space of Pseudomonas quinolone signal analogs as privileged structures and report the discovery of a thioquinolone as a potent inhibitor of the important virulence factor elastase of the human pathogen Pseudomonas aeruginosa. We provide evidence that the derivative binds to t...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2016-01, Vol.52 (92), p.13440-13443
Hauptverfasser: Szamosvári, Dávid, Reichle, Valentin F, Jureschi, Monica, Böttcher, Thomas
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Sprache:eng
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Zusammenfassung:We explore the chemical space of Pseudomonas quinolone signal analogs as privileged structures and report the discovery of a thioquinolone as a potent inhibitor of the important virulence factor elastase of the human pathogen Pseudomonas aeruginosa. We provide evidence that the derivative binds to the active site zinc of elastase and additionally acts as a fluorescent zinc sensor.
ISSN:1359-7345
1364-548X
DOI:10.1039/c6cc06295d