649757-53-9Relevant articles and documents
Exploring the chemical space of ureidothiophene-2-carboxylic acids as inhibitors of the quorum sensing enzyme PqsD from Pseudomonas aeruginosa
Sahner, J. Henning,Empting, Martin,Kamal, Ahmed,Weidel, Elisabeth,Groh, Matthias,B?rger, Carsten,Hartmann, Rolf W.
supporting information, p. 14 - 21 (2015/04/22)
Pseudomonas aeruginosa employs a quorum sensing (QS) communication system that makes use of small diffusible molecules. Among other effects, the QS system coordinates the formation of biofilm which decisively contributes to difficulties in the therapy of
Combining in silico and biophysical methods for the development of pseudomonas aeruginosa quorum sensing inhibitors: An alternative approach for structure-based drug design
Sahner, J. Henning,Brengel, Christian,Storz, Michael P.,Groh, Matthias,Plaza, Alberto,Müller, Rolf,Hartmann, Rolf W.
, p. 8656 - 8664 (2013/12/04)
The present work deals with the optimization of an inhibitor of PqsD, an enzyme essential for Pseudomonas aeruginosa quorum sensing apparatus. Molecular docking studies, supported by biophysical methods (surface plasmon resonance, isothermal titration cal
Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors
Baxter, Andrew,Brough, Steve,Cooper, Anne,Floettmann, Eike,Foster, Steve,Harding, Christine,Kettle, Jason,McInally, Tom,Martin, Craig,Mobbs, Michelle,Needham, Maurice,Newham, Pete,Paine, Stuart,St-Gallay, Steve,Salter, Sylvia,Unitt, John,Xue, Yafeng
, p. 2817 - 2822 (2007/10/03)
A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22.