Szamosvári Dávid, Reichle Valentin F, Jureschi Monica, Böttcher Thomas
Department of Chemistry, Konstanz Research School Chemical Biology, University of Konstanz, 78457 Konstanz, Germany.
Chem Commun (Camb). 2016 Nov 10;52(92):13440-13443. doi: 10.1039/c6cc06295d.
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.
我们探索了喹诺酮信号类似物作为优势结构的化学空间,并报告发现了一种硫代喹诺酮作为人类病原体铜绿假单胞菌重要毒力因子弹性蛋白酶的有效抑制剂。我们提供证据表明,该衍生物与弹性蛋白酶的活性位点锌结合,并额外充当荧光锌传感器。