226259-79-6Relevant academic research and scientific papers
PYRIDYLPYRROLE DERIVATIVES
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, (2008/06/13)
Object: to provide compounds having an inhibitory effect on the production of inflammatory cytokines. Constitution: compounds having general formula (I), pharmacologically acceptable salts thereof or derivatives of the same, wherein A: single bond, oxygen
Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase
Liverton, Nigel J.,Butcher, John W.,Claiborne, Christopher F.,Claremon, David A.,Libby, Brian E.,Nguyen, Kevin T.,Pitzenberger, Steven M.,Selnick, Harold G.,Smith, Garry R.,Tebben, Andrew,Vacca, Joseph P.,Varga, Sandor L.,Agarwal, Lily,Dancheck, Kim,Forsyth, Amy J.,Fletcher, Daniel S.,Frantz, Betsy,Hanlon, William A.,Harper, Coral F.,Hofsess, Scott J.,Kostura, Matthew,Lin, Jiunn,Luell, Sylvie,O'Neill, Edward A.,Orevillo, Chad J.,Pang, Margaret,Parsons, Janey,Rolando, Anna,Sahly, Yousif,Visco, Denise M.,O'Keefe, Stephen J.
, p. 2180 - 2190 (2007/10/03)
Novel potent and selective diarylimidazole inhibitors of p38 MAP (mitogen-activated protein) kinase are described which have activity in both cell-based assays of tumor necrosis factor-α (TNF-α) release and an animal model of rheumatoid arthritis. The SAR
Regulation of stress-induced cytokine production by pyridinylimidazoles inhibition of CSBP kinase
Gallagher, Timothy F.,Seibel, George L.,Kassis, Shouki,Laydon, Jeffrey T.,Blumenthal, Mary Jane,Lee, John C.,Lee, Dennis,Boehm, Jeffrey C.,Fier-Thompson, Susan M.,Abt, Jeffrey W.,Soreson, Margaret E.,Smietana, Juanita M.,Hall, Ralph F.,Garigipati, Ravi S.,Bender, Paul E.,Erhard, Karl F.,Krog, Arnold J.,Hofmann, Glenn A.,Sheldrake, Peter L.,McDonnell, Peter C.,Kumar, Sanjay,Young, Peter R.,Adams, Jerry L.
, p. 49 - 64 (2007/10/03)
Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway. Based upon SAR and protein homology modeling, the pharmacophore and three potential modes of binding to the enzyme are presented. For a subset of pyridinylimidazoles, binding is shown to correlate with inhibition of CSBP kinase activity, whereas no significant inhibition of PKA, PKα and ERK kinase activity is observed.
