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Bioorg Med Chem Lett. 2008 Jul 15;18(14):3959-62. doi: 10.1016/j.bmcl.2008.06.009. Epub 2008 Jun 10.

Discovery of selective and nonpeptidic cathepsin S inhibitors.

Author information

1
Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan. osamu.irie@novartis.com

Abstract

Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an in-house pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats.

PMID:
18572405
DOI:
10.1016/j.bmcl.2008.06.009
[Indexed for MEDLINE]

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