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Bioorg Med Chem Lett ; 13(19): 3243-6, 2003 Oct 06.
Article in English | MEDLINE | ID: mdl-12951101

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.


Subject(s)
Enzyme Inhibitors/chemical synthesis , Matrix Metalloproteinase Inhibitors , Metalloendopeptidases/antagonists & inhibitors , Piperazines/chemical synthesis , Tumor Necrosis Factor-alpha/metabolism , ADAM Proteins , ADAM17 Protein , Animals , Collagenases/metabolism , Enzyme Inhibitors/pharmacology , Matrix Metalloproteinase 13 , Metalloendopeptidases/metabolism , Piperazines/pharmacology , Rats
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