Abstract
We synthesized bicyclic thiophenes and 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives, and evaluated for their ability to inhibit LPS-stimulated production of TNF-alpha. Several compounds revealed excellent in vivo activity. Furthermore, an effective compound was found in adjuvant-induced arthritic model (AIA) of rat.
MeSH terms
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Animals
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Arthritis, Experimental / drug therapy
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Bridged Bicyclo Compounds / chemical synthesis
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Bridged Bicyclo Compounds / pharmacology
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Disease Models, Animal
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Inhibitory Concentration 50
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Lipopolysaccharides / antagonists & inhibitors
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Lipopolysaccharides / pharmacology
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacology*
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Rats
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Structure-Activity Relationship
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Thiophenes / chemical synthesis*
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Thiophenes / pharmacology*
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Tumor Necrosis Factor-alpha / antagonists & inhibitors*
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Tumor Necrosis Factor-alpha / biosynthesis
Substances
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Bridged Bicyclo Compounds
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Lipopolysaccharides
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Pyridines
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Thiophenes
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Tumor Necrosis Factor-alpha