Abstract
Anthranilic acid derivatives bearing basic amines were prepared and evaluated in vitro and in vivo as inhibitors of MMP-1, MMP-9, MMP-13, and TACE. Piperazine 4u has been identified as a potent, selective, orally active inhibitor of MMP-9 and MMP-13.
MeSH terms
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ADAM Proteins
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ADAM17 Protein
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Amines / chemistry*
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Animals
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Binding Sites
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Collagenases / metabolism
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Hydroxamic Acids / chemistry
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Interleukin-1
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Interleukin-1beta
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Magnetic Resonance Spectroscopy
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Matrix Metalloproteinase 1 / metabolism
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Matrix Metalloproteinase 13
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Matrix Metalloproteinase 9 / metabolism
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Matrix Metalloproteinase Inhibitors*
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Metalloendopeptidases
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Mice
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Models, Molecular
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Osteoarthritis / drug therapy
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Rats
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Structure-Activity Relationship
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ortho-Aminobenzoates / chemical synthesis
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ortho-Aminobenzoates / chemistry
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ortho-Aminobenzoates / pharmacology*
Substances
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Amines
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Enzyme Inhibitors
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Hydroxamic Acids
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Interleukin-1
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Interleukin-1beta
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Matrix Metalloproteinase Inhibitors
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ortho-Aminobenzoates
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ADAM Proteins
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Collagenases
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Matrix Metalloproteinase 13
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Metalloendopeptidases
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Mmp13 protein, mouse
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Mmp13 protein, rat
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Matrix Metalloproteinase 9
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Matrix Metalloproteinase 1
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ADAM17 Protein
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Adam17 protein, mouse
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Adam17 protein, rat