Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.

Richard M Angell, Tony D Angell, Paul Bamborough, David Brown, Murray Brown, Jacky B Buckton, Stuart G Cockerill, Chris D Edwards, Katherine L Jones, Tim Longstaff, Penny A Smee, Kathryn J Smith, Don O Somers, Ann L Walker, Malcolm Willson

Index: Bioorg. Med. Chem. Lett. 18(1) , 324-8, (2008)

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Abstract

The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38alpha are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model.