Synthetic quinolone signal analogues inhibiting the virulence factor elastase of Pseudomonas aeruginosa.
Dávid SzamosváriValentin F ReichleMonica JureschiThomas BöttcherPublished in: Chemical communications (Cambridge, England) (2018)
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.
Keyphrases
- pseudomonas aeruginosa
- biofilm formation
- cystic fibrosis
- acinetobacter baumannii
- endothelial cells
- molecular docking
- candida albicans
- oxide nanoparticles
- small molecule
- signaling pathway
- escherichia coli
- staphylococcus aureus
- quantum dots
- induced pluripotent stem cells
- high throughput
- high resolution
- living cells
- drug resistant
- mass spectrometry
- water soluble
- structure activity relationship