Your browser doesn't support javascript.
loading
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness, Shaun R; Devraj, Rajesh V; Devadas, Balekudru; Walker, John K; Boehm, Terri L; Durley, Richard C; Shieh, Huey; Xing, Li; 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; Messing, Dean; Yang, Jerry; Mao, Michael K; Yalamanchili, Gopi; Vonder Embse, Richard; Hirsch, Jeffrey; Saabye, Matthew; Bonar, Sheri; Webb, Elizabeth; Anderson, Gary; Monahan, Joseph B.
Affiliation
  • Selness SR; Department of Medicinal Chemistry, Pfizer Corporation, 700 Chesterfield Parkway West, Chesterfield, MO 63017, United States. shaun.selness@gmail.com
Bioorg Med Chem Lett ; 21(13): 4066-71, 2011 Jul 01.
Article in En | MEDLINE | ID: mdl-21641211
ABSTRACT
The synthesis and SAR studies of a novel N-aryl pyridinone class of p38 kinase inhibitors are described. Systematic structural modifications to the HTS lead, 5, led to the identification of (-)-4a as a clinical candidate for the treatment of inflammatory diseases. Additionally, the chiral synthesis and properties of (-)-4a are described.
Subject(s)
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Pyrones / Benzamides / P38 Mitogen-Activated Protein Kinases / Enzyme Inhibitors Limits: Animals / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Type: Article Affiliation country: United States
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Pyrones / Benzamides / P38 Mitogen-Activated Protein Kinases / Enzyme Inhibitors Limits: Animals / Humans / Male Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2011 Type: Article Affiliation country: United States