Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2006 Jun 1;16(11):2909-14. Epub 2006 Mar 20.

Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.

Author information

1
Celera Genomics, Inc., 180 Kimball Way, South San Francisco, CA 94080, USA. jim.palmer@celera.com

Abstract

We have prepared a series of cathepsin K inhibitors bearing the keto-1,3,4-oxadiazole warhead capable of forming a hemithioketal complex with the target enzyme. By modifying binding moieties at the P1, P2, and prime side positions of the inhibitors, we have achieved selectivity over cathepsins B, L, and S, and have achieved sub-nanomolar potency against cathepsin K. This series thus represents a promising chemotype that could be used in diseases implicated by imbalances in cathepsin K activity such as osteoporosis.

PMID:
16546382
DOI:
10.1016/j.bmcl.2006.03.001
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center