Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR

The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure–activity relationships of the series against p38α 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.

Graphical abstractStructure–activity relationships of the biphenyl amide (BPA) series against p38α are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a selective compound showing oral activity in an in vivo disease model.Figure optionsDownload full-size imageDownload as PowerPoint slide