Abstract
Investigation of furans, pyrroles and pyrazolones identified 3-pyridyl-2,5-diaryl-pyrroles as potent, orally bioavailable inhibitors of p38 kinase. 3-(4-pyridyl-2-(4-fluoro-phenyl)-5-(4-methylsulfinylphenyl)-pyrrol e (L-167307) reduces secondary paw swelling in the rat adjuvant arthritis model: ID50 = 7.4 mg/kg/b.i.d.
MeSH terms
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Animals
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Arthritis, Experimental / drug therapy
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Calcium-Calmodulin-Dependent Protein Kinases / antagonists & inhibitors*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology*
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Furans / chemical synthesis
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Furans / pharmacokinetics
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Furans / pharmacology*
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Humans
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Mitogen-Activated Protein Kinases*
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Pyrazoles / chemical synthesis
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Pyrazoles / pharmacokinetics
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Pyrazoles / pharmacology*
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Pyrroles / chemical synthesis
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Pyrroles / pharmacokinetics
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Pyrroles / pharmacology*
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Rats
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p38 Mitogen-Activated Protein Kinases
Substances
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Enzyme Inhibitors
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Furans
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Pyrazoles
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Pyrroles
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Calcium-Calmodulin-Dependent Protein Kinases
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Mitogen-Activated Protein Kinases
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p38 Mitogen-Activated Protein Kinases