Non-peptidic inhibitors of human neutrophil elastase: The design and synthesis of sulfonanilide-containing inhibitors
| Autor: | Masanori Kawamura, Yoshisuke Nakayama, Okada Takanori, Katsuhiro Imaki, Takaaki Amino, Yasuhiro Sakai, Kaoru Kobayashi, Tetsuya Mohri, Hisao Nakai, Yuuki Nagao |
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| Rok vydání: | 1996 |
| Předmět: |
Male
Cell Membrane Permeability Serine Proteinase Inhibitors Human neutrophil Neutrophils Stereochemistry Guinea Pigs Clinical Biochemistry Glycine Pharmaceutical Science Biochemistry Substrate Specificity Sulfonanilide Structure-Activity Relationship chemistry.chemical_compound Animal model Drug Discovery Animals Humans Molecular Biology Chromatography High Pressure Liquid Sulfonamides Aniline Compounds Chemistry Organic Chemistry Elastase Benzene derivatives Molecular Medicine Leukocyte Elastase |
| Zdroj: | Bioorganic & Medicinal Chemistry. 4:2115-2134 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/s0968-0896(96)00216-7 |
| Popis: | A novel series of pivaloyloxy benzene derivatives has been identified as potent and selective human neutrophil elastase (HNE) inhibitors. Convergent syntheses were developed in order to identify the inhibitors which are intravenously effective in an animal model. A compound of particular interest is the sulfonanilide-containing analogues. Structure-activity relationships are discussed. Structural requirements for metabolic stabilization are also discussed. |
| Databáze: | OpenAIRE |
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