Almtraet--The results of a structure-activity relationship study focusing on the interaction of a series of phthalimide and saccharin derivatives with leukocyte elastase, cathepsin G and proteinase 3 are described. The phthalimide derivatives were found to be inactive while some of the saccharin der
Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3
โ Scribed by William C. Groutas; Michael J. Brubaker; Lee S. Chong; Radhika Venkataraman; He Huang; Jeffrey B. Epp; Rongze Kuang; John R. Hoidal
- Publisher
- Elsevier Science
- Year
- 1995
- Tongue
- English
- Weight
- 572 KB
- Volume
- 3
- Category
- Article
- ISSN
- 0968-0896
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โฆ Synopsis
Structure-activity relationship study and in vitro biochemical studies with human leukocyte elastase, cathepsin G and proteinase 3 were conducted using a series of succinimide derivatives.
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The inhibitory activity toward human leukocyte elastase (HLE), cathepsin G (Cat G), and proteinase 3 (PR 3) of a series of saccharin derivatives having a sulfinate leaving group was investigated. The results of this study revealed that (a) inhibitory activity is dependent on the nature and pKa of th
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