Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 18, Pages 7928-7934Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00875
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Funding
- NIH [GM57481]
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Weak partial agonists that promote a desensitized state of the alpha 7 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 alpha 7 nAChR.
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