Synthesis and AChE inhibitory activity of N -glycosyl benzofuran derivatives

Six N -glycosyl benzofuran derivatives were synthesized by the catalysis of organic bases and condensation agents. The benzofuran derivatives were obtained by the reaction of various salicylaldehydes in acetone, and then hydrolyzed to the corresponding carboxylic acids. Finally, the target compounds...

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Bibliographic Details
Published in:Heterocyclic communications 2019-12, Vol.25 (1), p.162
Main Authors: Wu, Yu-Ran, Ren, Shu-Ting, Wang, Lei, Liu, Xiu-Jian, Wang, You-Xian, Liu, Shu-Hao, Liu, Wei-Wei, Shi, Da-Hua, Cao, Zhi-Ling
Format: Article
Language:English
Subjects:
Acetone
Acylation
Carboxylic acids
Chemical synthesis
Derivatives
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Summary:Six N -glycosyl benzofuran derivatives were synthesized by the catalysis of organic bases and condensation agents. The benzofuran derivatives were obtained by the reaction of various salicylaldehydes in acetone, and then hydrolyzed to the corresponding carboxylic acids. Finally, the target compounds were synthesized by acylation and the reaction conditions were optimized. The acetylcholinesterase (AChE) inhibitory activity of the desired compounds was tested using Ellman’s method. Most of the compounds showed acetylcholinesterase-inhibition activity; N -(2,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2 H -pyran-3-yl)benzofuran-2-carbxamide ( 5a ) showed the best acetylcholinesterase inhibition, with an inhibitory rate of 84%.
ISSN:0793-0283
2191-0197
DOI:10.1515/hc-2019-0021