Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
Article Details
- CitationCopy to clipboard
Moss N, Xiong Z, Burke M, Cogan D, Gao DA, Haverty K, Heim-Riether A, Hickey ER, Nagaraja R, Netherton M, O'Shea K, Ramsden P, Schwartz R, Shih DT, Ward Y, Young E, Zhang Q
Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
Bioorg Med Chem Lett. 2012 Dec 1;22(23):7189-93. doi: 10.1016/j.bmcl.2012.09.054. Epub 2012 Oct 2.
- PubMed ID
- 23084902 [ View in PubMed]
- Abstract
This paper details exploration of a class of triazole-based cathepsin S inhibitors originally reported by Ellman and co-workers. SAR studies involving modifications across the whole inhibitor provide a perspective on the strengths and weaknesses of this class of inhibitors. In addition, we put the unique characteristics of this class of compounds into perspective with other classes of cathepsin S inhibitors.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) N-[(1S)-2-[(4-cyano-1-methylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-oxoethyl]morpholine-4-carboxamide Cathepsin S IC 50 (nM) 1.5 N/A N/A Details N-[(1S)-2-[(4-cyano-1-methylpiperidin-4-yl)amino]-1-(cyclohexylmethyl)-2-oxoethyl]morpholine-4-carboxamide Cathepsin S IC 50 (nM) 0.9 N/A N/A Details