851317-54-9Relevant academic research and scientific papers
Ketoheterocycle-based inhibitors of cathepsin K: A novel entry into the synthesis of peptidic ketoheterocycles
Tavares, Francis X.,Deaton, David N.,Miller, Aaron B.,Miller, Larry R.,Wright, Lois L.
, p. 3891 - 3895 (2007/10/03)
Ketoheterocyclic inhibitors of cathepsin K have been disclosed. SAR of potency enhancing P2-P3 groups coupled with ketoheterocyclic warheads to provide cathepsin K inhibitors have been described. In addition, a novel route to access
Novel and potent cyclic cyanamide-based cathepsin K inhibitors
Deaton, David N.,Hassell, Anne M.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Shewchuk, Lisa M.,Tavares, Francis X.,Willard Jr., Derril H.,Wright, Lois L.
, p. 1815 - 1819 (2007/10/03)
Starting from a PDE IV inhibitor hit derived from high throughput screening of the compound collection, a key pyrrolidine cyanamide pharmacophore was identified. Modifications of the pyrrolidine ring produced enhancements in cathepsin K inhibition. An X-r
Acyclic cyanamide-based inhibitors of cathepsin K
Barrett, David G.,Deaton, David N.,Hassell, Anne M.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Payne, J. Alan,Shewchuk, Lisa M.,Willard Jr., Derril H.,Wright, Lois L.
, p. 3039 - 3043 (2007/10/03)
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.
