Synthesis of imperatorin analogs and their evaluation as acetylcholinesterase and butyrylcholinesterase inhibitors.
In this study, we synthesized several imperatorin analogs using imperatorin and xanthotoxin as substrates. The anti-cholinesterase activities of all compounds were evaluated in in vitro experiments according to the modified Ellman's method. For each synthesized compound, IC50 values for both enzymes were established. Galantamine hydrobromide was used as a positive control in the enzymatic experiments. All active compounds showed selectivity toward butyrylcholinesterase (BuChE) rather than acetylcholinesterase. The most active ones were 8-(3-methylbutoxy)-psoralen and 8-hexoxypsoralen with IC50 values for BuChE of around 16.5 and 16.4 µM, respectively. The results of our study may be considered as the beginning of a search for potential anti-Alzheimer's disease drugs based on the structure of natural furocoumarins.
['Granica|Sebastian|S|', 'Kiss|Anna K|AK|', 'Jarończyk|Małgorzata|M|', 'Maurin|Jan K|JK|', 'Mazurek|Aleksander P|AP|', 'Czarnocki|Zbigniew|Z|']
D000110:Acetylcholinesterase D000544:Alzheimer Disease D000818:Animals D001665:Binding Sites D002091:Butyrylcholinesterase D002800:Cholinesterase Inhibitors D011564:Furocoumarins D005702:Galantamine D062105:Molecular Docking Simulation D013329:Structure-Activity Relationship
Acetylcholinesterase Butyrylcholinesterase Furocoumarins Alzheimer's disease Angelica archangelica