Abstract
We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addition results in improve potencies against p38.
MeSH terms
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Allosteric Site
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Amides / chemistry*
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Anti-Inflammatory Agents / pharmacology
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Chemistry, Pharmaceutical / methods
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Cytokines / metabolism
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Humans
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Inflammation / drug therapy
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Inhibitory Concentration 50
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Ketones / chemistry*
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Models, Chemical
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Models, Molecular
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
Substances
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Amides
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Anti-Inflammatory Agents
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Cytokines
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Enzyme Inhibitors
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Ketones
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p38 Mitogen-Activated Protein Kinases