Zobrazeno 1 - 3
of 3
pro vyhledávání: '"Danielle K. Wiener"'
Autor:
Lars Karlsson, Neelakandha S. Mani, Todd K. Jones, Steven Nguyen, Pragnya J. Desai, Cheryl A. Grice, Kristen L. Arienti, Robin L. Thurmond, Frank U. Axe, James P. Edwards, Mike Randal, Siquan Sun, Danielle K. Wiener, Michael K. Ameriks, Jing Liu, Alice Lee-Dutra, Damara Gebauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2370-2374
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 a
Autor:
Cheryl A. Grice, Todd K. Jones, Scott D. Bembenek, Lars Karlsson, Siquan Sun, James P. Edwards, Danielle K. Wiener, Alice Lee-Dutra, Steven Nguyen, Robin L. Thurmond
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
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 connectivi
Autor:
John J. M. Wiener, Siquan Sun, Alvah T. Wickboldt, James P. Edwards, Todd K. Jones, Danielle K. Wiener, Lars Karlsson, Alice Lee-Dutra, Steven Nguyen, Cheryl A. Grice
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
A novel class of tetrahydropyrido-pyrazole thioether amines that display potency against human Cathepsin S have been previously reported. Here, further SAR investigations of the P3, P4, and P5 regions are described. In particular, 4-fluoropiperidine