Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists
Autor: | Wei He, Yong Gong, Guy Van Lommen, Jean Pierre Frans Van Wauwe, J. Kent Barbay, Concha Claes, Pamela J. Hornby, Mieke Buntinx, Jian Li |
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Rok vydání: | 2008 |
Předmět: |
Molecular Structure
Stereochemistry Chemistry Histiocytic lymphoma Organic Chemistry Clinical Biochemistry Pharmaceutical Science Tumor cells Biochemistry Chemical synthesis C5a receptor Structure-Activity Relationship Liver metabolism Drug Discovery Microsomes Liver Quinolines Humans Molecular Medicine Structure–activity relationship Amines Receptor Receptor Anaphylatoxin C5a Molecular Biology |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 18:2544-2548 |
ISSN: | 0960-894X |
Popis: | A novel series of substituted 2-aryl-5-amino-5,6,7,8-tetrahydroquinoline C5a receptor antagonists is reported. Synthetic routes were developed that allow the substituents on the tetrahydroquinoline core to be efficiently varied, facilitating determination of structure-activity relationships. Members of the series display high binding affinity for the C5a receptor and are potent functional antagonists. |
Databáze: | OpenAIRE |
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