The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT sub(2C) receptor agonist
5-HT sub(2C) agonists have shown efficacy in limiting food consumption and thus may serve as an important drug class in combating obesity. We describe the design and synthesis of a novel tricyclic single-nitrogen scaffold that was used to produce 5-HT sub(2C) agonists. SAR was developed around this...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-01, Vol.16 (15), p.4130-4134 |
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| Sprache: | eng |
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| container_end_page | 4134 |
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| container_issue | 15 |
| container_start_page | 4130 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 16 |
| creator | Huck, Bayard R Llamas, Luis Robarge, Michael J Dent, Thomas C Song, Jianping Hodnick, William F Crumrine, Chris Stricker-Krongrad, Alain Harrington, John Brunden, Kurt R Bennani, Youssef L |
| description | 5-HT sub(2C) agonists have shown efficacy in limiting food consumption and thus may serve as an important drug class in combating obesity. We describe the design and synthesis of a novel tricyclic single-nitrogen scaffold that was used to produce 5-HT sub(2C) agonists. SAR was developed around this chemotype and compounds were identified that were potent (K sub(i) - 15 nM) and selective relative to other 5-HT sub(2) receptors. The most promising compound displayed a good pharmacokinetic profile in multiple animal species, and was efficacious in an acute feeding study in rats. |
| doi_str_mv | 10.1016/j.bmcl.2006.04.070 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2006-01, Vol.16 (15), p.4130-4134 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_17211179 |
| source | ScienceDirect Journals (5 years ago - present) |
| title | The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT sub(2C) receptor agonist |
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