Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives
| Autor: | Radhika Venkataraman, William C. Groutas, He Huang, Jeffrey B. Epp, Lee S. Chong, Nadene Houser-Archield, Jerald J. McClenahan |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Cathepsin G
Structure-Activity Relationship chemistry.chemical_compound Saccharin Hydroxylamine Drug Discovery medicine Humans Structure–activity relationship chemistry.chemical_classification Pancreatic Elastase biology Serine Endopeptidases Elastase Biological activity Cathepsins Enzyme chemistry Mechanism of action Biochemistry Enzyme inhibitor biology.protein Molecular Medicine medicine.symptom Leukocyte Elastase |
| Zdroj: | Journal of Medicinal Chemistry. 36:3178-3181 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00073a019 |
| Popis: | A series of saccharin derivatives I has been synthesized and evaluated for their inhibitory activity toward human leukocyte elastase and cathepsin G. Most of the compounds were found to be efficient and time-dependent inhibitors of elastase. Inactivated elastase was found to regain its activity almost fully after 24 h (80-90% activity) and the half-lives of reactivation ranged between 12-15 h. Addition of hydroxylamine to fully-inactivated enzyme led to rapid and complete recovery of enzymatic activity. A tentative mechanism of action is proposed on the basis of biochemical and model studies. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|