Abstract
A series of benzodiazepine MMP/TACE inhibitors bearing polar moieties has been synthesized in an effort to optimize inhibitory activity against LPS-stimulated TNF production in human monocytes and oral activity in a murine LPS model.
MeSH terms
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ADAM Proteins
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ADAM17 Protein
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Animals
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Benzodiazepines / pharmacology*
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Cell Line
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology*
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Humans
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Lipopolysaccharides / pharmacology
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Matrix Metalloproteinase Inhibitors*
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Metalloendopeptidases / antagonists & inhibitors*
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Mice
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Mice, Inbred BALB C
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Monocytes / drug effects
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Monocytes / metabolism
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Mouth / drug effects
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Tumor Necrosis Factor-alpha / biosynthesis
Substances
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Enzyme Inhibitors
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Lipopolysaccharides
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Matrix Metalloproteinase Inhibitors
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Tumor Necrosis Factor-alpha
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Benzodiazepines
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ADAM Proteins
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Metalloendopeptidases
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ADAM17 Protein
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ADAM17 protein, human
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Adam17 protein, mouse