Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective α-sulfone hydroxamates
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- 作者：Stephen A. Kolodziej ; Susan L. Hockerman ; Terri L. Boehm ; Jeffery N. Carroll ; Gary A. DeCrescenzo ; Joseph J. McDonald ; Debbie A. Mischke ; Grace E. Munie ; Theresa R. Fletcher ; Joseph G. Rico ; Nathan W.
- 关键词：Matrix metalloproteinase inhibitor ; MMP inhibitor ; MMP-13 selective ; Hydroxamate ; MMP-1/14 dual-sparing ; Metalloenzyme
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 June 2010
- 年：2010
- 卷：20
- 期：12
- 页码：3557-3560
- 全文大小：409 K
文摘
A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats.