N-糖基苯并呋喃衍生物的合成及其乙酰胆碱酯酶抑制活性

IF 1.3 3区化学 Q3 CHEMISTRY, ORGANIC

Heterocyclic Communications Pub Date : 2019-01-01 DOI:10.1515/hc-2019-0021

Yu-Ran Wu, Shu-Ting Ren, Lei Wang, Xiu-Jian Liu, You-Xian Wang, Shu-Hao Liu, Wei-wei Liu, D. Shi, Zhi-ling Cao

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引用次数: 1

摘要

摘要以有机碱和缩合剂为催化剂，合成了6个n -糖基苯并呋喃衍生物。以各种水杨醛在丙酮中反应得到苯并呋喃衍生物，然后水解得到相应的羧酸。最后通过酰化反应合成了目标化合物，并对反应条件进行了优化。采用Ellman法测定化合物的乙酰胆碱酯酶(AChE)抑制活性。大部分化合物具有抑制乙酰胆碱酯酶的活性;N-(2,4,5-三羟基-6-(羟甲基)四氢- 2h -吡喃-3-酰基)苯并呋喃-2-卡伯沙酰胺(5a)对乙酰胆碱酯酶的抑制效果最好，抑制率为84%。

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Synthesis and AChE inhibitory activity of N-glycosyl benzofuran derivatives

Abstract 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-2H-pyran-3-yl)benzofuran-2-carbxamide (5a) showed the best acetylcholinesterase inhibition, with an inhibitory rate of 84%.

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来源期刊

Heterocyclic Communications 化学-有机化学

CiteScore

3.80

自引率

4.30%

发文量

审稿时长

1.4 months

期刊介绍： Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.