| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375869 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of 5-(piperidinylethyloxy)quinoline 5-HT1 receptor ligands have been studied by elaboration of the series of dual 5-HT1-SSRIs reported previously. These new compounds display a different in vitro pharmacological profile with potent affinity across the 5-HT1A, 5-HT1B and 5-HT1D receptors and selectivity against the serotonin transporter. Furthermore, they have improved pharmacokinetic profiles and CNS penetration.
Graphical abstractSAR studies on a series of substituted phenyl piperazines and piperidines are described. Several examples are disclosed as potent 5-HT1 receptor ligands and their PK profiles presented.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Simon E. Ward, Peter Eddershaw, Sean T. Flynn, Laurie Gordon, Peter J. Lovell, Susan H. Moore, Claire M. Scott, Paul W. Smith, Kevin M. Thewlis, Paul A. Wyman,