Abstract
A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.
MeSH terms
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Animals
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Anti-Inflammatory Agents / administration & dosage
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology
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Cell Line
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Glucocorticoids / administration & dosage
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Glucocorticoids / chemistry*
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Glucocorticoids / pharmacology
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Heterocyclic Compounds / administration & dosage
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Heterocyclic Compounds / chemistry*
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Heterocyclic Compounds / pharmacology
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Humans
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Lipopolysaccharides / pharmacology
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Mice
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Mice, Inbred C57BL
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Rats
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Tumor Necrosis Factor-alpha / biosynthesis
Substances
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Anti-Inflammatory Agents
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Glucocorticoids
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Heterocyclic Compounds
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Lipopolysaccharides
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Tumor Necrosis Factor-alpha