Portal de Periódicos da CAPES

N-Arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B

2003; Elsevier BV; Volume: 13; Issue: 22 Linguagem: Inglês

10.1016/j.bmcl.2003.08.006

1464-3405

Paul D. Greenspan, Kirk Clark, Scott D. Cowen, Leslie W. McQuire, Rubén Tommasi, David Farley, Elizabeth Quadros, David E. Coppa, Zengming Du, Fang Zheng, Huanghai Zhou, John Doughty, Karen Toscano, Andrew M. Wigg, Siyuan Zhou,

Calpain Protease Function and Regulation

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.