Document Report Card
Basic Information
ID: ALA1136448
Journal: Bioorg Med Chem Lett
Title: N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Authors: Greenspan PD, Clark KL, Cowen SD, McQuire LW, Tommasi RA, Farley DL, Quadros E, Coppa DE, Du Z, Fang Z, Zhou H, Doughty J, Toscano KT, Wigg AM, Zhou S.
Abstract: To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P(2)-P(3) amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and selective inhibitors with excellent oral availability.
CiteXplore: 14592520