181630-93-3Relevant articles and documents
Role of the hydrogen bonding heteroatom-lys53 interaction between the p38r mitogen-activated protein (map) kinase and pyridinyl-substituted 5-membered heterocyclic ring inhibitors
Thaher, Bassam Abu,Koch, Pierre,Schattel, Verena,Laufer, Stefan
supporting information; experimental part, p. 2613 - 2617 (2010/02/28)
In the framework of investigating the role of heteroatoms in pyridinyl-substituted 5-membered (hetero)cycles as potential p38α MAP kinase inhibitor scaffolds, cyclopentene, pyrrole, furan, and imidazole analogues were synthesized and tested with respect t
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 Map kinase inhibitors
Revesz, Laszlo,Di Padova, Franco E.,Buhl, Thomas,Feifel, Roland,Gram, Hermann,Hiestand, Peter,Manning, Ute,Zimmerlin, Alfred G.
, p. 1261 - 1264 (2007/10/03)
The 4-hydroxypiperidine substituent was found to confer high p38 selectivity devoid of COX-1 affinity, when attached to a series of pyridinyl substituted heterocycles. Pyridinyloxazole 11 showed a promising in vivo profile with bioavailability of 64% and
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
