Abstract
C-Jun NH2 terminal kinases (JNKs) are important cell signaling enzymes. JNK1 plays a central role in linking obesity and insulin resistance. JNK2 and JNK3 may be involved in inflammatory and neurological disorders, respectively. Small-molecule JNK inhibitors could be valuable tools to study the therapeutic benefits of inhibiting these enzymes and as leads for potential drugs targeting JNKs. In this report, we disclose a series of potent and highly selective JNK inhibitors with good pharmacokinetic profiles.
MeSH terms
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Administration, Oral
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Amides / chemical synthesis*
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Amides / pharmacokinetics
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Amides / pharmacology
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Animals
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Biological Availability
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Crystallography, X-Ray
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Humans
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In Vitro Techniques
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JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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Mice
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Microsomes / metabolism
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Models, Molecular
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Pyridines / chemical synthesis*
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Pyridines / pharmacokinetics
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Pyridines / pharmacology
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Rats
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Structure-Activity Relationship
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Thermodynamics
Substances
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Amides
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Pyridines
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JNK Mitogen-Activated Protein Kinases