Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction.
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ABSTRACT:
SUBMITTER: Young S
PROVIDER: S-EPMC2864113 | biostudies-literature | 2010 May
REPOSITORIES: biostudies-literature
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Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction.
Young Sherri S Fabio Karine K Guillon Christophe C Mohanta Pramod P Halton Timothy A TA Heck Diane E DE Flowers Robert A RA Laskin Jeffrey D JD Heindel Ned D ND
Bioorganic & medicinal chemistry letters 20100303 9
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 ...[more]
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