| Literature DB >> 15896958 |
David G Barrett1, David N Deaton, Anne M Hassell, Robert B McFadyen, Aaron B Miller, Larry R Miller, J Alan Payne, Lisa M Shewchuk, Derril H Willard, Lois L Wright.
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.Entities:
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Year: 2005 PMID： 15896958 DOI： 10.1016/j.bmcl.2005.04.032
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823