Sulfonium as a Surrogate for Ammonium: A New ?7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.
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ABSTRACT:
SUBMITTER: Quadri M
PROVIDER: S-EPMC5653211 | biostudies-literature | 2017 Sep
REPOSITORIES: biostudies-literature
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Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.
Quadri Marta M Stokes Clare C Gulsevin Alican A Felts Ashley C J ACJ Abboud Khalil A KA Papke Roger L RL Horenstein Nicole A NA
Journal of medicinal chemistry 20170914 18
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 interact ...[more]
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