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Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43.

Acyclic cyanamide-based inhibitors of cathepsin K.

Author information

1
Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.

Abstract

Conversion of the proline-derived cyanamide lead to an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large increase in inhibitory activity. An X-ray structure of a co-crystal of a cyanamide with cathepsin K confirmed the enzyme interaction. Furthermore, a representative acyclic cyanamide inhibitor 6r was able to attenuate bone resorption in the rat calvarial model.

PMID:
15896958
DOI:
10.1016/j.bmcl.2005.04.032
[Indexed for MEDLINE]

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