Abstract
A series of novel MMP-13 and TNF-alpha converting enzyme inhibitors based on piperazine 2-hydroxamic acid scaffolds are described. The TACE, MMP-1 and MMP-13 activity of these inhibitors as well as the effect of substitution of the piperazine nitrogen and the P-1' benzyloxy tailpiece is discussed. Moderate in vivo activity is observed with several members of this group.
MeSH terms
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ADAM Proteins
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ADAM17 Protein
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Animals
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Collagenases / metabolism
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Matrix Metalloproteinase 13
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Matrix Metalloproteinase Inhibitors*
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Metalloendopeptidases / antagonists & inhibitors*
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Metalloendopeptidases / metabolism
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Piperazines / chemical synthesis*
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Piperazines / pharmacology
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Rats
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Tumor Necrosis Factor-alpha / metabolism*
Substances
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Enzyme Inhibitors
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Matrix Metalloproteinase Inhibitors
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Piperazines
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Tumor Necrosis Factor-alpha
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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, rat
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ADAM17 Protein
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Adam17 protein, rat