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Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.

Bioorganic & medicinal chemistry letters (2007-11-06)
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
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.

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Sigma-Aldrich
3-Bromo-4-methylbenzoic acid, technical grade, 85%