Amino Derivatives of Acridine: Synthesis and Study of Anticholinesterase and Antioxidant Activity

IF 0.8 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Doklady Chemistry Pub Date : 2023-06-28 DOI:10.1134/S0012500823700167
A. V. Shchepochkin, A. F. Uglova, I. A. Utepova, E. S. Gradoblyanskaya, M. A. Averkov, N. V. Kovaleva, E. V. Rudakova, N. P. Boltneva, O. G. Serebryakova, G. F. Makhaeva,  V. N. Charushin,  O. N. Chupakhin
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Abstract

A simple and feasible approach to the synthesis of new amine derivatives of acridine based on the methodology of direct C–H functionalization has been developed. The inhibitory effect of the synthesized compounds toward cholinesterases and carboxylesterase as well as their antioxidant activity have been studied. A high anti-BChE activity has been shown for N-methylpiperazine derivative promising for further optimization to design on its basis new series of compounds efficient for the treatment of neurodegenerative diseases.

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吖啶的氨基衍生物:抗胆碱酯酶和抗氧化活性的合成与研究
提出了一种简单可行的基于碳氢直接官能化方法合成新的吖啶胺类衍生物的方法。研究了合成的化合物对胆碱酯酶和羧酸酯酶的抑制作用及其抗氧化活性。n -甲基哌嗪衍生物具有较高的抗bche活性,有望在其基础上进一步优化设计出治疗神经退行性疾病的新系列化合物。
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来源期刊
Doklady Chemistry
Doklady Chemistry 化学-化学综合
CiteScore
1.20
自引率
12.50%
发文量
7
审稿时长
6-12 weeks
期刊介绍: Doklady Chemistry is a journal that publishes new research in chemistry and chemical engineering of great significance. Initially the journal was a forum of the Russian Academy of Science and published only best contributions from Russia in the form of short articles. Now the journal welcomes submissions from any country in the English or Russian language. Every manuscript must be recommended by Russian or foreign members of the Russian Academy of Sciences.
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