2,3-吲哚齐墩果酸及其衍生物的合成及胆碱酯酶抑制效能

IF 0.6 Q4 CHEMISTRY, ORGANIC

Molbank Pub Date : 2023-10-18 DOI:10.3390/m1739

Anastasiya V. Petrova, Irina V. Zueva, Konstantin A. Petrov

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引用次数: 0

摘要

本文综述了前人和新合成的含C28位七元环胺齐墩果酸衍生物的合成及其生物活性。通过1H和13C NMR对化合物进行了全面表征，并采用Ellman 's法对化合物的生物活性进行了评价。其中2,3-吲哚齐墩果酸对乙酰胆碱酯酶活性最强，IC50值为0.78µM。由于齐墩果酸，特别是吲哚衍生物对乙酰胆碱酯酶和丁基胆碱酯酶的抑制作用研究有限，因此这些结果具有重要意义。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Synthesis and Cholinesterase Inhibitory Potency of 2,3-Indolo-oleanolic Acid and Some Related Derivatives

In this study, the synthesis and biological activities of previously and newly synthesized oleanolic acid derivatives containing seven-membered cyclic amines at the C28 position were described. The obtained compounds were fully characterized via 1H and 13C NMR spectroscopy, and the bioactivity was evaluated by Ellman’s method. Among the tested compounds, 2,3-indolo-oleanolic acid was found to be the most active compound with an IC50 value of 0.78 µM against acetylcholinesterase. These results are significant due to the fact that research on the inhibition of acetylcholinesterase and butyrylcholinesterase enzymes by oleanolic acid, in particular indoloderivatives, is limited.

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来源期刊

Molbank Chemistry-Physical and Theoretical Chemistry

CiteScore

0.70

自引率

33.30%

发文量

174

审稿时长

11 weeks

期刊介绍： •organic synthesis •biosynthesis •extraction and purification •natural product derivatives •structural elucidation (X-ray crystallography, NMR, etc.)