1049094-63-4Relevant academic research and scientific papers
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: Part 1
Lee-Dutra, Alice,Wiener, Danielle K.,Arienti, Kristen L.,Liu, Jing,Mani, Neelakandha,Ameriks, Michael K.,Axe, Frank U.,Gebauer, Damara,Desai, Pragnya J.,Nguyen, Steven,Randal, Mike,Thurmond, Robin L.,Sun, Siquan,Karlsson, Lars,Edwards, James P.,Jones, Todd K.,Grice, Cheryl A.
scheme or table, p. 2370 - 2374 (2010/07/20)
A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety may bind to the S3 pocket of the enzyme. Additional optimization led to the discovery of aminoethylthioethers with improved enzymatic activity and submicromolar cellular potency.
