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  • Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines.

Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines.

Bioorganic chemistry (2017-10-11)
Alireza Basiri, Basma M Abd Razik, Mohammed Oday Ezzat, Yalda Kia, Raju Suresh Kumar, Abdulrahman I Almansour, Natarajan Arumugam, Vikneswaran Murugaiyah
摘要

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 IC

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1,3-亚丙基丙烯, 99%