Design and synthesis of butynyloxyphenyl β-sulfone piperidine hydroxamates as TACE inhibitors
| Autor: | Yi Zhu, Yuhua Zhang, Jeremy I. Levin, LinHong Sun, Mila T. Du, Kaapjoo Park, Alexis Aplasca |
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| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Pharmaceutical Science ADAM17 Protein Matrix metalloproteinase Biochemistry Chemical synthesis Sulfone Mice Structure-Activity Relationship chemistry.chemical_compound Piperidines In vivo Drug Discovery Animals Potency Structure–activity relationship Molecular Biology chemistry.chemical_classification Hydroxamic acid biology Organic Chemistry General Medicine Combinatorial chemistry In vitro ADAM Proteins Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Piperidine Selectivity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 16:3927-3931 |
| ISSN: | 0960-894X |
| Popis: | A series of butynyloxyphenyl beta-sulfone piperidine hydroxamate TACE inhibitors was designed and synthesized. The resulting structure-activity relationship and MMP selectivity of the series were examined. Of the compounds investigated, 17s has excellent in vitro potency against isolated TACE enzyme, shows good selectivity over MMP-1, -2, -7, -8, -9, -13, and -14, and oral activity in an in vivo mouse model of TNF-alpha production. |
| Databáze: | OpenAIRE |
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