Conjugates of Tacrine with Aminomethylidene-Substituted Malonates: Synthesis and Biological Evaluation

被引：1

作者：

Grishchenko, M. V. ^{[1
]}

Elkina, N. A. ^{[1
]}

Makhaeva, G. F. ^{[2
]}

Burgart, Ya. V. ^{[1
]}

Boltneva, N. P. ^{[2
]}

Rudakova, E. V. ^{[2
]}

Shchegolkov, E. V. ^{[1
]}

Kovaleva, N. V. ^{[2
]}

Serebryakova, O. G. ^{[2
]}

Saloutin, V. I. ^{[1
]}

机构：

[1] Russian Acad Sci, Postovsky Inst Organ Synth, Ural Branch, Ekaterinburg 620990, Russia

[2] Russian Acad Sci, Inst Physiol Act Cpds, Fed Res Ctr Problem Chem Phys & Med Chem, Chernogolovka 142432, Russia

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2022年 / 92卷 / 11期

基金：

俄罗斯基础研究基金会;

关键词：

conjugate; tacrine; diethylmalonate; anticholinesterase activity; propidium displacement; ALZHEIMERS-DISEASE; INHIBITORS; CHOLINESTERASE; ACETYLCHOLINESTERASE; DERIVATIVES; ANTIOXIDANT; HYBRIDS;

D O I：

10.1134/S1070363222110093

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The condensation of tacrine aminopolymethylene derivatives with diethyl (ethoxymethylidene)malonate led to the new hybrid compounds-conjugates, which were the effective inhibitors of acetylcholinesterase (AChE) (IC50 up to 0.538 mu M) and butyrylcholinesterase (IC50 up to 0.0314 mu M). They can displace propidium iodide from peripherical anionic site of AChE at the level of the reference drug donepezil and demonstrate a weak antioxidant activity. Conjugates are of interest for further extended research as potential drugs for the Alzheimer's disease treatment.

引用

页码：2259 / 2266

页数：8

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