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

被引：1

作者：

Petrova, Anastasiya V. ^{[1
]}

Zueva, Irina V. ^{[2
]}

Petrov, Konstantin A. ^{[2
]}

机构：

[1] Russian Acad Sci, Ufa Inst Chem, Ufa Fed Res Ctr, 71 Prospect Octyabrya, Ufa 450054, Russia

[2] Russian Acad Sci, Arbuzov Inst Organ & Phys Chem, FRC Kazan Sci Ctr, 8 St Academician Arbuzov, Kazan 420088, Russia

来源：

MOLBANK | 2023年 / 2023卷 / 04期

基金：

俄罗斯科学基金会;

关键词：

oleanolic acid; indolo-triterpenoids; homopiperazine; acetylcholinesterase; butyrylcholinesterase; neurodegenerative diseases; Alzheimer's disease; POTENTIAL INHIBITORS;

D O I：

10.3390/M1739

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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 mu M 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.

引用

页数：7

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