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ID: ALA1136235

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors.

Authors: Letavic MA, Barberia JT, Carty TJ, Hardink JR, Liras J, Lopresti-Morrow LL, Mitchell PG, Noe MC, Reeves LM, Snow SL, Stam EJ, Sweeney FJ, Vaughn ML, Yu CH.

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.

CiteXplore: 12951101

DOI: 10.1016/s0960-894x(03)00666-8