Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
| Autor: | Yong Gong, Guy Van Lommen, Jian Li, Concha Claes, Wei He, Pamela J. Hornby, Mieke Buntinx, J. Kent Barbay, Jean Pierre Frans Van Wauwe |
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| Rok vydání: | 2008 |
| Předmět: |
Aniline Compounds
Molecular model Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Ligands Biochemistry C5a receptor Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Aniline Drug Discovery Side chain Humans Structure–activity relationship Receptor Anaphylatoxin C5a Molecular Biology chemistry.chemical_classification Binding Sites Molecular Structure Organic Chemistry Aromatic amine Biological activity Models Chemical chemistry Drug Design Quinolines Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 18:3852-3855 |
| ISSN: | 0960-894X |
| Popis: | A series of aniline-substituted tetrahydroquinoline C5a receptor antagonists were discovered. A functionality requirement of ortho substitution on the aniline was revealed. Secondary anilines, in general, outperformed tertiary analogs in inhibition of C5a-induced calcium mobilization. Further enhancement of activity was realized in the presence of an ortho hydroxyalkyl side chain. The functional IC(50) of selected analogs was optimized to the single-digit nanomolar level. |
| Databáze: | OpenAIRE |
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