口服生物利用度双重 MMP-1/MMP-14 节约型、MMP-13 选择性 α-砜羟酰胺。
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
机构信息
Department of Medicinal Chemistry, Pfizer Research & Development, St. Louis, MO 63198, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3557-60. doi: 10.1016/j.bmcl.2010.04.130. Epub 2010 May 23.
PMID:20529684
Abstract
A series of phenyl piperidine alpha-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.
摘要
已经利用溶液相和树脂结合文库技术的组合制备了一系列苯基哌啶α-亚砜羟胺衍生物，得到了对 MMP-13 具有高活性和高选择性的化合物，对 MMP-1 和 MMP-14（MT1-MMP）具有双重保护作用，并在大鼠中具有口服生物利用度。
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