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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1
Alice Lee-Dutra1, Danielle K Wiener, Kristen L Arienti
1Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. alee7@its.jnj.com
Bioorganic & Medicinal Chemistry Letters
|February 16, 2010
Abstract:
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.
