Abstract
Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1beta stimulated synovial fibroblasts. The 2-amino-5-chloropyridine-4-carboxamides were identified as the most potent inhibitors with improved cellular activity.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.
MeSH terms
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Amides / chemistry
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Amides / pharmacology
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Amino Acid Sequence
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Aminopyrine / chemistry*
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Aminopyrine / pharmacology*
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Anti-Inflammatory Agents / chemistry*
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Anti-Inflammatory Agents / pharmacology*
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Arthritis, Rheumatoid / drug therapy
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Fibroblasts / drug effects
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Fibroblasts / immunology
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Humans
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I-kappa B Kinase / antagonists & inhibitors*
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I-kappa B Kinase / metabolism
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I-kappa B Proteins / chemistry
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Interleukin-1beta / antagonists & inhibitors*
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Interleukin-1beta / metabolism
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Joint Capsule / cytology
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Molecular Sequence Data
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Structure-Activity Relationship
Substances
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Amides
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Anti-Inflammatory Agents
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I kappa B beta protein
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I-kappa B Proteins
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Interleukin-1beta
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Aminopyrine
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I-kappa B Kinase