649757-53-9Relevant academic research and scientific papers
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.
, 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
Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: Structure-based optimization of a virtual screening hit
Sahner, J. Henning,Groh, Matthias,Negri, Matthias,Haupenthal, J?rg,Hartmann, Rolf W.
, p. 223 - 231 (2013/10/01)
Rising resistance against current antibiotics necessitates the development of antibacterial agents with alternative targets. The "switch region" of RNA polymerase (RNAP), addressed by the myxopyronins, could be such a novel target site. Based on a hit can
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
Synthesis of novel 2-thienylimino-1,3-thiazolidin-4-ones
Abdillahi, Ismail,Revelant, Germain,Datoussaid, Yazid,Kirsch, Gilbert
experimental part, p. 2543 - 2546 (2010/09/08)
The preparation of new 2-thienylimino-1,3-thiazolidin-4-ones from 3-aminothiophene-2-carboxylate using an easy four-step procedure is described. Georg Thieme Verlag Stuttgart New York.
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.
