1224508-84-2Relevant academic research and scientific papers
UNIQUE DUAL-ACTION THERAPEUTICS
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Page/Page column 29; 30, (2010/05/14)
A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n = 0, 1; X = C, Si, and N+ and NSAID = ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed
Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction
Young, Sherri,Fabio, Karine,Guillon, Christophe,Mohanta, Pramod,Halton, Timothy A.,Heck, Diane E.,Flowers II, Robert A.,Laskin, Jeffrey D.,Heindel, Ned D.
supporting information; experimental part, p. 2987 - 2990 (2010/08/19)
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.
