Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity
| Autor: | Ashley C. Felts, Marta Quadri, Khalil A. Abboud, Clare Stokes, Roger L. Papke, Nicole A. Horenstein, Alican Gulsevin |
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| Rok vydání: | 2017 |
| Předmět: |
Models
Molecular 0301 basic medicine alpha7 Nicotinic Acetylcholine Receptor Isostere Sulfonium Stereochemistry Morpholines Sulfonium Compounds Partial agonist Article Xenopus laevis 03 medical and health sciences chemistry.chemical_compound Onium Compounds α7 nicotinic acetylcholine receptor Ammonium Compounds Drug Discovery Animals Humans Ammonium Nicotinic Agonists Chemistry 030104 developmental biology Nicotinic agonist Molecular Medicine Pharmacophore Trifluoromethanesulfonate |
| Zdroj: | Journal of Medicinal Chemistry. 60:7928-7934 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | Weak partial agonists that promote a desensitized state of the α7 nicotinic acetylcholine receptor (nAChR) have been associated with anti-inflammatory effects. Exemplar compounds feature a tertiary or quaternary ammonium group. We report the synthesis, structure, and electrophysiological evaluation of 1-ethyl-4-phenylthiomorpholin-1-ium triflate, a weak partial agonist with a sulfonium isostere of the ammonium pharmacophore. These results offer new insights in understanding nAChR-ligand interactions and provide a new chemical space to target the α7 nAChR. |
| Databáze: | OpenAIRE |
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