Promising Drug Discovery for Choline Derivatives via Ugi Reaction and their Inhibition Activity on AChE Enzyme
Abstract
A great focus was given to multi-component reactions in the last two decades because many compounds were synthesized through them and approved biological and pharmacological properties. The two famous reactions are Passerini (3-CR) and Ugi (4-CR). From this point, we started our study to modify choline derivatives and to study their inhibitory effect on AchE enzyme (acetylcholinesterase enzyme). We synthesized four different compounds by Ugi reaction (2b,2c,2d), all of them were new after that, they were tested for the inhibitory activity through the screening kit k-197 all of them gave activity, but the strength of activity was different the most active one was compound 2b and the others gave inhibitory effect but not in the same potency than the relative activity% (RA%) and relative inhibitory% (RI%). Donepezil was used as standard, and linear plots were drawn to compare activity with donepezil.Keywords:
AChE, Alzheimer disease, Bis amides, Carbamates, Inhibition, MCRS, NMR, ScreeningReferences
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