Download MendeleyExploration of the P(2)-P(3) SAR of aldehyde cathepsin K inhibitors
Boros, E.E., Deaton, D.N., Hassell, A.M., McFadyen, R.B., Miller, A.B., Miller, L.R., Paulick, M.G., Shewchuk, L.M., Thompson, J.B., Willard Jr., D.H., Wright, L.L.(2004) Bioorg Med Chem Lett 14: 3425-3429
- PubMed: 15177446
- DOI: https://doi.org/10.1016/j.bmcl.2004.04.084
- Primary Citation of Related Structures:
1SNK - PubMed Abstract:
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 600 nM and 130 pM.
Organizational Affiliation:
Department of Medicinal Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
