| Title : Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction - Young_2010_Bioorg.Med.Chem.Lett_20_2987 |
| Author(s) : Young S , Fabio K , Guillon C , Mohanta P , Halton TA , Heck DE , Flowers RA, 2nd , Laskin JD , Heindel ND |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :2987 , 2010 |
|
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. |
| PubMedSearch : Young_2010_Bioorg.Med.Chem.Lett_20_2987 |
| PubMedID: 20347302 |
Young S, Fabio K, Guillon C, Mohanta P, Halton TA, Heck DE, Flowers RA, 2nd, Laskin JD, Heindel ND (2010)
Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction
Bioorganic & Medicinal Chemistry Lett
20 :2987
Young S, Fabio K, Guillon C, Mohanta P, Halton TA, Heck DE, Flowers RA, 2nd, Laskin JD, Heindel ND (2010)
Bioorganic & Medicinal Chemistry Lett
20 :2987