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.
Neil Moss  1 ,  Zhaoming Xiong ,  Mike Burke ,  Derek Cogan ,  Donghong A Gao ,  Kathleen Haverty ,  Alexander Heim-Riether ,  Eugene R Hickey ,  Raj Nagaraja ,  Matthew Netherton ,  Kathy O'Shea ,  Philip Ramsden ,  Racheline Schwartz ,  Daw-Tsun Shih ,  Yancey Ward ,  Erick Young ,  Qing Zhang
Affiliations
  • 1. Department of Medicinal Chemistry, Immunology and Inflammation, Boehringer Ingelheim Pharmaceutical, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA. [email protected]
PMID: 23084902 DOI: 10.1016/j.bmcl.2012.09.054
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.

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