Synthesis and Biological Evaluation of 1,3,4-Oxadiazole Derivatives as Acetylcholinesterase Inhibitors

A series of 1,3,4-oxadiazole derivatives were designed, synthesized, and evaluated as acetylcholin­esterase inhibitors. Their structure was confirmed by IR, NMR, and high-resolution mass spectra. The syn­thesized compounds showed significant acetylcholinesterase inhibitory activity with an IC 50 val...

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Published in:Russian journal of organic chemistry 2022-10, Vol.58 (10), p.1520-1526
Main Authors: Yang, Shun, Zou, Jing-Pei, Li, Xiang-Rong, Li, Rui, Qian, Jing-Jing, Wu, Wen-Long, Su, Jia-Bin, Chen, Ke-Qi, Qin, Tian, Liu, Shan-Ming, Liu, Wei-Wei, Shi, Da-Hua
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Language:English
Subjects:
Amino acids
Chemistry
Chemistry and Materials Science
Inhibitors
Mass spectra
Molecular docking
NMR
Nuclear magnetic resonance
Organic Chemistry
Oxadiazoles
Synthesis
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container_title Russian journal of organic chemistry
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creator Yang, Shun
Zou, Jing-Pei
Li, Xiang-Rong
Li, Rui
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Chen, Ke-Qi
Qin, Tian
Liu, Shan-Ming
Liu, Wei-Wei
Shi, Da-Hua
description A series of 1,3,4-oxadiazole derivatives were designed, synthesized, and evaluated as acetylcholin­esterase inhibitors. Their structure was confirmed by IR, NMR, and high-resolution mass spectra. The syn­thesized compounds showed significant acetylcholinesterase inhibitory activity with an IC 50 value of 0.07 μM for the most potent compound. Molecular docking study of the most active compound indicated that it interacted with the crucial amino acids present at the catalytic active site and peripheral anionic site of acetylcholinesterase. The results suggested that the obtained 1,3,4-oxadiazole derivatives may be the potential drug candidates for the treatment of Alzheimer’s disease as AChE inhibitors.
doi_str_mv 10.1134/S1070428022100207
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subjects Amino acids
Chemistry
Chemistry and Materials Science
Inhibitors
Mass spectra
Molecular docking
NMR
Nuclear magnetic resonance
Organic Chemistry
Oxadiazoles
Synthesis
title Synthesis and Biological Evaluation of 1,3,4-Oxadiazole Derivatives as Acetylcholinesterase Inhibitors
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