| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376561 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
A novel series of pyridyl-phenyl ethers are disclosed, which possess dual 5-HT and NA reuptake pharmacology with good selectivity over dopamine reuptake inhibition. An analysis of the relationship between lipophilicity and pharmacology highlighted that potent dual SNRI activity was only achievable at c log P > 3.5. The series was found to possess significant polypharmacology issues, and we concluded that this off-target promiscuity was related to lipophilicity.
Graphical abstractA novel series of pyridyl-phenyl ethers are disclosed, which possess potent dual 5-HT and NA reuptake pharmacology with good selectivity over dopamine reuptake inhibition. The series was found to possess significant polypharmacology issues, we concluded that this off-target promiscuity was related to high lipophilicity.Figure optionsDownload full-size imageDownload as PowerPoint slide
