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Bioorg Med Chem Lett. 2010 Apr 1;20(7):2370-4. doi: 10.1016/j.bmcl.2010.01.108. Epub 2010 Jan 28.

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.

Author information

1
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. alee7@its.jnj.com

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.

PMID:
20153648
DOI:
10.1016/j.bmcl.2010.01.108
[Indexed for MEDLINE]

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