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  • Title: Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines.
    Author: Basiri A, Abd Razik BM, Ezzat MO, Kia Y, Kumar RS, Almansour AI, Arumugam N, Murugaiyah V.
    Journal: Bioorg Chem; 2017 Dec; 75():210-216. PubMed ID: 28987876.
    Abstract:
    Alzheimer's disease (AD) is a prevalent neurodegenerative disorder, which affected 35 million people in the world. The most practiced approach to improve the life expectancy of AD patients is to increase acetylcholine neurotransmitter level at cholinergic synapses by inhibition of cholinesterase enzymes. A series of unreported piperidone grafted spiropyrrolidines 8(a-p) were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Therein, compounds 8h and 8l displayed more potent AChE enzyme inhibition than standard drug with IC50 values of 1.88 and 1.37 µM, respectively. Molecular docking simulations for 8l possessing the most potent AChE inhibitory activities, disclosed its interesting binding templates to the active site channel of AChE enzymes. These compounds are remarkable AChE inhibitors and have potential as AD drugs.
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