Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement
| Autor: | Neil Moss, Racheline Schwartz, Erick R. R. Young, Michael J. Burke, Eugene R. Hickey, Matthew R. Netherton, Raj Nagaraja, Yancey David Ward, Alexander Heim-Riether, Kathleen Haverty, Derek Cogan, Daw-Tsun Shih, Philip D. Ramsden, Qing Zhang, Gao Donghong A, Zhaoming Xiong, Kathy O’Shea |
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| Rok vydání: | 2012 |
| Předmět: |
Chemistry
Stereochemistry Organic Chemistry Clinical Biochemistry Triazole Pharmaceutical Science Thiophenes Metabolic stability Triazoles Biochemistry Amides Cathepsins chemistry.chemical_compound Structure-Activity Relationship Amide Drug Discovery Microsomes Liver Molecular Medicine Humans Protease Inhibitors Molecular Biology Cathepsin S Half-Life Protein Binding |
| Zdroj: | Bioorganicmedicinal chemistry letters. 22(23) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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