Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists
| Autor: | Yoshihide Tomata, Mariko Hirozane, Tatsuhiko Fujimoto, Jun Kunitomo, Shogo Marui |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Receptors
Neuropeptide Chemistry Drug discovery digestive oral and skin physiology Organic Chemistry Clinical Biochemistry Orexin hypocretin Pharmaceutical Science Pharmacology Ligands Biochemistry Orexin receptor Receptors G-Protein-Coupled Piperidines nervous system Orexin Receptors mental disorders Drug Discovery Molecular Medicine Receptor Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:6409-6413 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.08.094 |
| Popis: | To generate novel human Orexin-2 Receptor (OX2R) antagonists, a spiropiperidine based scaffold was designed and a SAR study was carried out. Compound 4f possessed the highest OX2R antagonistic activity with an IC(50) value of 3nM with 450-fold selectivity against Orexin-1 Receptor (OX1R). |
| Databáze: | OpenAIRE |
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