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Discovery of PH-797804, a Highly Selective and Potent Inhibitor of p38 MAP Kinase

Shaun R Selness, 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, etc.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71.

PMID: 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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP586379660 PH-797804 PH-797804 586379-66-0 Price
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