Exploration of cathepsin S inhibitors characterized by a triazole P1–P2 amide replacement

This paper details exploration of a class of triazole-based cathepsin S inhibitors examplified by compound 6 originally reported by Ellman and coworkers. SAR studies involving modifications across the whole inhibitor provide a perspective on the strengths and weaknesses of this class of inhibitors. 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.