Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
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Date
2014-01
Authors
Basiri, Alireza
Journal Title
Journal ISSN
Volume Title
Publisher
Universiti Sains Malaysia
Abstract
Alzheimer’s disease (AD) is the most common form of dementia among the elderly
people. Based on the cholinergic hypothesis, loss of cholinergic neurons in AD patients’
brain leads to the decline of acetylcholine (ACh) neurotransmitter level and eventually
causes severe dysfunctions in the cholinergic neurotransmission. Thus, increasing the
ACh levels is a promising therapeutic approach to restore the substantial impairment of
memory and cognitive dysfunctions in AD patients. The search for new cholinesterase
inhibitors is still ongoing worldwide. Inspired by the biological significance of
pyrimidine-grafted derivatives, especially in cholinesterase inhibition, seventy-four
novel pyrimidine embedded derivatives, namely pyridopyrimidines 6(a-l),
pyridopyrimidothiones 7(a-l), N-ethyl-pyridopyrimidothiones 8(a-j), N-ethylmorpholino
pyridopyrimidothiones 9(a-j), pyrimidinethiols 11(a-l) and thiazolopyrimidines 13(a-r)
were synthesized and evaluated for their cholinesterases inhibitory potential against
acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
Description
Keywords
Piperidone-Grafted Pyrimidine , Thiazolopyrimidine