| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372737 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel.
Graphical abstractA knowledge based approach was applied to explore novel NOP receptor agonists with simplified hydrophobes. Compound 51 was identified as a high affinity, potent NOP receptor agonist.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ronald Palin, John K. Clark, Louise Evans, Helen Feilden, Dan Fletcher, Niall M. Hamilton, Andrea K. Houghton, Philip S. Jones, Duncan McArthur, Brian Montgomery, Paul D. Ratcliffe, Alasdair R.C. Smith, Aaron Sutherland, Mark A. Weston, Grant Wishart,