1049103-12-9Relevant articles and documents
Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors
Wiener, Danielle K.,Lee-Dutra, Alice,Bembenek, Scott,Nguyen, Steven,Thurmond, Robin L.,Sun, Siquan,Karlsson, Lars,Grice, Cheryl A.,Jones, Todd K.,Edwards, James P.
scheme or table, p. 2379 - 2382 (2010/07/14)
A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide functional groups were prepared with the goal of improving upon the cellular activity of amidoethylthioethers. This Letter describes altered amide connectivity, in conjunction with changes to other binding elements, resulting in improved potency, as well as increased knowledge of the relationship between this chemotype and human CatS activity.