| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366967 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
A rational structure–activity relationship study around compound (1) is reported. The lead optimisation programme led to the identification of sulfonamide (25), a molecule combining dopamine D2/D3 receptor antagonism with serotonin 5-HT2A, 5-HT2C, 5-HT6 receptor antagonism for an effective treatment of schizophrenia. Compound (25) was shown to possess the required in vivo activity with no EPS liability.
Graphical abstractThe SAR study around compound (1), led to the identification of sulfonamide (25), a molecule combining dopamine D2/D3 receptor antagonism with serotonin 5-HT2A, 5-HT2C, 5-HT6 receptor antagonism to treat schizophrenia.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
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Authors
Vincenzo Garzya, Ian T. Forbes, Andrew D. Gribble, Mike S. Hadley, Andrew P. Lightfoot, Andrew H. Payne, Alexander B. Smith, Sara E. Douglas, David G. Cooper, Ian G. Stansfield, Malcom Meeson, Emma E. Dodds, Declan N.C. Jones, Martyn Wood,