| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370429 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
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 IC50 value of 3 nM with 450-fold selectivity against Orexin-1 Receptor (OX1R).
Graphical abstractTo 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 IC50 value of 3 nM with 450-fold selectivity against Orexin-1 Receptor (OX1R).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Tatsuhiko Fujimoto, Yoshihide Tomata, Jun Kunitomo, Mariko Hirozane, Shogo Marui,