Abstract
The biphenyl amides (BPAs) are a novel series of p38alpha 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.
MeSH terms
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Administration, Oral
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Animals
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Benzamides / blood
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Benzamides / chemical synthesis*
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Benzamides / chemistry
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Benzamides / pharmacology*
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Biphenyl Compounds / blood
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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacology*
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Combinatorial Chemistry Techniques
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Crystallography, X-Ray
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Disease Models, Animal
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Mitogen-Activated Protein Kinase 14 / antagonists & inhibitors*
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Molecular Conformation
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Molecular Structure
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Protein Kinase Inhibitors / blood
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Rats
Substances
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Benzamides
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Biphenyl Compounds
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Protein Kinase Inhibitors
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Mitogen-Activated Protein Kinase 14