Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective α-sulfone hydroxamates
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. Stehle、Craig Swearingen、Daniel P. Becker
DOI:10.1016/j.bmcl.2010.04.130
日期:2010.6
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. (C) 2010 Elsevier Ltd. All rights reserved.