2. Academic Validation
  3. Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase

Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase

  • Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71. doi: 10.1016/j.bmcl.2011.04.121.
Shaun R Selness 1,  Rajesh V Devraj,  Balekudru Devadas,  John K Walker,  Terri L Boehm,  Richard C Durley,  Huey Shieh,  Li Xing,  Paul V Rucker,  Kevin D Jerome,  Alan G Benson,  Laura D Marrufo,  Heather M Madsen,  Jeff Hitchcock,  Tom J Owen,  Lance Christie,  Michele A Promo,  Brian S Hickory,  Edgardo Alvira,  Win Naing,  Radhika Blevis-Bal,  Dean Messing,  Jerry Yang,  Michael K Mao,  Gopi Yalamanchili,  Richard Vonder Embse,  Jeffrey Hirsch,  Matthew Saabye,  Sheri Bonar,  Elizabeth Webb,  Gary Anderson,  Joseph B Monahan
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Pfizer Corporation, 700 Chesterfield Parkway West, Chesterfield, MO 63017, United States. [email protected]
PMID: 21641211 DOI: 10.1016/j.bmcl.2011.04.121
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.

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