Abstract
A series of pyrazolo[1,5-a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described.
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis
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Anti-Inflammatory Agents / pharmacology
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Area Under Curve
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Chemistry, Pharmaceutical / methods*
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Dogs
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Drug Design
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacokinetics*
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Humans
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Inhibitory Concentration 50
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Leukocytes, Mononuclear / drug effects
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MAP Kinase Signaling System
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Pyridines / chemical synthesis*
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Pyridines / pharmacokinetics
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Rats
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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p38 Mitogen-Activated Protein Kinases / metabolism
Substances
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Anti-Inflammatory Agents
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Enzyme Inhibitors
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Pyridines
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p38 Mitogen-Activated Protein Kinases