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Published on: March 29, 2017
Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction
Sherri Young1, Karine Fabio, Christophe Guillon
1Department of Chemistry, Lehigh University, Bethlehem, PA 18015, USA.
Abstract:
The design and study of two classes of noncompetitive acetylcholinesterase inhibitors (AChEIs) which also function as NSAID prodrugs are reported. The most potent AChEIs disclosed contain an aromatic alkyl-aryl linker between an NSAID and a lipophilic choline mimic and they inhibit acetylcholinesterase (AChE) in the submicromolar range. These agents have the therapeutic potential to dually target inflammation by releasing an NSAID in vivo and activating the cholinergic anti-inflammatory pathway via cholinergic up-regulation.
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