586377-72-2Relevant academic research and scientific papers
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase
Selness, Shaun R.,Boehm, Terri L.,Walker, John K.,Devadas, Balekudru,Durley, Richard C.,Kurumbail, Ravi,Shieh, Huey,Xing, Li,Hepperle, Michael,Rucker, Paul V.,Jerome, Kevin D.,Benson, Alan G.,Marrufo, Laura D.,Madsen, Heather M.,Hitchcock, Jeff,Owen, Tom J.,Christie, Lance,Promo, Michele A.,Hickory, Brian S.,Alvira, Edgardo,Naing, Win,Blevis-Bal, Radhika,Devraj, Rajesh V.,Messing, Dean,Schindler, John F.,Hirsch, Jeffrey,Saabye, Matthew,Bonar, Sheri,Webb, Elizabeth,Anderson, Gary,Monahan, Joseph B.
, p. 4059 - 4065 (2011/08/02)
A series of N-aryl pyridinone inhibitors of p38 mitogen activated protein (MAP) kinase were designed and prepared based on the screening hit SC-25028 (1) and structural comparisons to VX-745 (5). The focus of the investigation targeted the dependence of potency and metabolic stability on the benzyloxy connectivity, the role of the C-6 position and the substitution pattern on the N-phenyl ring. Further optimization produced the highly selective and potent pyridinones 2 and 3. These inhibitors exhibited activity in both acute and chronic models of inflammation.
