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Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity |
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| Authors: | Angell Richard Aston Nicola M Bamborough Paul Buckton Jacky B Cockerill Stuart deBoeck Suzanne J Edwards Chris D Holmes Duncan S Jones Katherine L Laine Dramane I Patel Shila Smee Penny A Smith Kathryn J Somers Don O Walker Ann L |
| Affiliation: | aGlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK |
| Abstract: | The biphenyl amides (BPAs) are a novel series of p38α MAP kinase inhibitor. The optimisation of the series to give compounds that are potent in an in vivo disease model is discussed. SAR is presented and rationalised with reference to the crystallographic binding mode. |
| Keywords: | p38 Kinase p38 Alpha p38 CSBP MAP kinase Inhibitors Biphenyl amide BPA Biphenyl amides BPAs Protein kinase X-ray structure Binding mode Structure-based drug design Kinase selectivity Structure– activity relationships PG-PS model CIA model |
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