Citation: Yu Xiang, Chen Yafang, Zhao Youfang, Huang Guojuan. Syntheses and Acetylcholinesterase Inhibitory Activities of 7-Diethylaminocoumarin-Based Hydrazone/Acylhydrazone Derivatives[J]. Chemistry, ;2020, 83(1): 92-95. shu

Syntheses and Acetylcholinesterase Inhibitory Activities of 7-Diethylaminocoumarin-Based Hydrazone/Acylhydrazone Derivatives

College of Pharmacy, Guizhou University of Traditional Chinese Medicne, Guiyang, 550025

Received Date: 3 August 2019
Accepted Date: 3 October 2019

Figures(1)

Thirteen 7-N, Ndiethylaminocoumarin-based hydrazone/acylhydrazone derivatives were synthesized from 7-N, Ndiethylamino-4-methylcoumarin via oxidation with SeO₂, and then reacting with substituted hydrazine and acylhydrazine by using the impregnation method. Their structures were confirmed by melting point, ¹H NMR and MS. Preliminary bioassay results showed that compounds 4a and 4c had potential inhibitory activity against acetylcholinesterase, and their IC₅₀ values were 42.89 and 90.32 μmol/L, respectively. The preliminary study on the structure-activity relationships indicated that acylhydrazone derivatives have better inhibitory activity against acetylcholinesterase than those of the hydrazone derivatives.
- Coumarin,
- Acetylcholinesterase inhibitor,
- Derivatives,
- Synthesis
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