Design, Green Synthesis, and Biological Evaluation of New Substituted Tetrahydropyrimidine Derivatives as Acetylcholinesterase Inhibitors

A series of novel tetrahydropyrimidin-4-yl)pyridine derivatives 6(a-h) have been designed and synthesized as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The chemical structures of all newly synthesized compounds were characterized by spectroscopic methods (IR, 1 H NMR...

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Bibliographic Details
Published in:Polycyclic aromatic compounds 2022-09, Vol.42 (8), p.5231-5241
Main Authors: Mariki, Ali akbar, Anaeigoudari, Akbar, Zahedifar, Mahboobeh, Pouramiri, Behjat, Ayati, Adileh, Lotfi, Safa
Format: Article
Language:English
Subjects:
Acetylcholinesterase
Alzheimer's disease
butyrylcholinesterase inhibitors
Chemical synthesis
Donepezil
Inhibitors
NMR
Nuclear magnetic resonance
Substitutes
tetrahydropyrimidin-4-yl)pyridine
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Summary:A series of novel tetrahydropyrimidin-4-yl)pyridine derivatives 6(a-h) have been designed and synthesized as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The chemical structures of all newly synthesized compounds were characterized by spectroscopic methods (IR, 1 H NMR, 13 C NMR) and elemental analyzes. The in vitro studies showed that all the synthesized derivatives showed significant BChE inhibitory activity more potent than donepezil as the standard (IC 50 values less than 0.1 µM). All the target compounds demonstrated good AChE inhibitory effects comparable with donepezil as the reference drug with IC 50 values ranging from 0.08 to 0.1 µM. The best results were obtained by 4-methyl substituted derivative 6d with IC 50 value of 0.082 µM which was comparable with AChE inhibitory effects of donepezil (IC 50  = 0.079 µM).
ISSN:1040-6638
1563-5333
DOI:10.1080/10406638.2021.1933102