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Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors |
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| Authors: | Letavic Michael A Barberia John T Carty Thomas J Hardink Joel R Liras Jennifer Lopresti-Morrow Lori L Mitchell Peter G Noe Mark C Reeves Lisa M Snow Sheri L Stam Ethan J Sweeney Francis J Vaughn Marcie L Yu Chul H |
| Affiliation: | Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. michael_a_letavic@groton.pfizer.com |
| 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. |
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