N-Arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B

详细信息    查看全文

• 作者：Greenspan ; Paul D. ; Clark ; Kirk L. ; Cowen ; Scott D. ; McQuire ; Leslie W. ; Tommasi ; Ruben A. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2003
• 出版时间：November 17, 2003
• 年：2003
• 卷：13
• 期：22
• 页码：4121-4124
• 全文大小：208 K

文摘

To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P₂–P₃ amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and selective inhibitors with excellent oral availability.