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Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-09-14 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00875
Marta Quadri 1, 2 , Clare Stokes 2 , Alican Gulsevin 1 , Ashley C. J. Felts 3 , Khalil A. Abboud 3 , Roger L. Papke 2 , Nicole A. Horenstein 1
Affiliation  

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.

中文翻译:

as作为铵的替代品:具有脱敏活性的新型α7烟碱乙酰胆碱受体部分激动剂。

促进α7烟碱乙酰胆碱受体(nAChR)脱敏状态的弱部分激动剂与抗炎作用有关。示例化合物具有叔或季铵基团。我们报告了1-乙基-4-苯基硫吗啉-1-三氟甲磺酸盐的合成,结构和电生理学评估,它是一种弱的部分激动剂,具有铵药效基团的sulf等排酮。这些结果为了解nAChR-配体相互作用提供了新的见识,并为靶向α7nAChR提供了新的化学空间。
更新日期:2017-09-14
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