736143-91-2Relevant articles and documents
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors
Boros, Eric E.,Deaton, David N.,Hassell, Anne M.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Paulick, Margot G.,Shewchuk, Lisa M.,Thompson, James B.,Willard Jr., Derril H.,Wright, Lois L.
, p. 3425 - 3429 (2007/10/03)
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600nM and 130pM.