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Bioorg Med Chem Lett. 2010 May 1;20(9):2987-90. doi: 10.1016/j.bmcl.2010.02.102. Epub 2010 Mar 3.

Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction.

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1
Department 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.

PMID:
20347302
PMCID:
PMC2864113
DOI:
10.1016/j.bmcl.2010.02.102
[Indexed for MEDLINE]
Free PMC Article
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