Synthesis and AChE inhibitory activity of N-glycosyl benzofuran derivatives

Heterocyclic communications

article

Yu-Ran Wu¹  Shu-Ting Ren¹  Lei Wang¹  Xiu-Jian Liu¹  You-Xian Wang¹  Shu-Hao Liu¹  Wei-Wei Liu¹  Da-Hua Shi¹  Zhi-Ling Cao¹ 

[1] College of Pharmaceutical Sciences, Huaihai Institute of Technology;Jiangsu Institute of Marine Resources;Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Huaihai Institute of Technology;Co-Innovation Center of Jiangsu Marine Bio-industry Technology

关键词: D-glucosamine;    amide;    anti-acetylcholinesterase;   

DOI  :  10.1515/hc-2019-0021

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

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%.

【 授权许可】

CC BY|CC BY-NC-ND