AMINO DERIVATIVES OF ACRIDINE: SYNTHESIS, STUDY OF ANTICHOLINESTERASE AND ANTIOXIDANT ACTIVITIES

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Abstract

A simple and accessible approach to the synthesis of new amine derivatives of acridine based on the direct C–H functionalization methodology was developed. The inhibitory effect of the synthesized compounds on cholinesterases and carboxylesterases, as well as their antioxidant activity, was studied. A moderate inhibition of BChE by the morpholine and pyrazole derivatives of acridine and a high anti-BChE activity of the N-methyl-piperazine one were shown.

About the authors

A. V. Shchepochkin

Institute of Organic Synthesis named by I.Y. Postovsky, Ural branch of the Russian Academy of Sciences; Ural Federal University named by the first President of Russia B.N. Yeltsin

Author for correspondence.
Email: avs@ios.uran.ru
Russian, 620219, Yekaterinburg; Russian, 620002, Yekaterinburg

V. N. Charushin

Institute of Organic Synthesis named by I.Y. Postovsky, Ural branch of the Russian Academy of Sciences; Ural Federal University named by the first President of Russia B.N. Yeltsin

Email: avs@ios.uran.ru
Russian, 620219, Yekaterinburg; Russian, 620002, Yekaterinburg

G. F. Makhaeva

Institute of Physiologically Active Substances of the Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry of the Russian Academy of Sciences

Email: avs@ios.uran.ru
Russian, 142432, Chernogolovka

O. G. Serebryakova

Institute of Physiologically Active Substances of the Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry of the Russian Academy of Sciences

Email: avs@ios.uran.ru
Russian, 142432, Chernogolovka

N. P. Boltneva

Institute of Physiologically Active Substances of the Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry of the Russian Academy of Sciences

Email: avs@ios.uran.ru
Russian, 142432, Chernogolovka

E. V. Rudakova

Institute of Physiologically Active Substances of the Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry of the Russian Academy of Sciences

Email: avs@ios.uran.ru
Russian, 142432, Chernogolovka

N. V. Kovaleva

Institute of Physiologically Active Substances of the Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry of the Russian Academy of Sciences

Email: avs@ios.uran.ru
Russian, 142432, Chernogolovka

M. A. Averkov

Institute of Organic Synthesis named by I.Y. Postovsky, Ural branch of the Russian Academy of Sciences; Ural Federal University named by the first President of Russia B.N. Yeltsin

Email: avs@ios.uran.ru
Russian, 620219, Yekaterinburg; Russian, 620002, Yekaterinburg

E. S. Gradoblyanskaya

Ural Federal University named by the first President of Russia B.N. Yeltsin

Email: avs@ios.uran.ru
Russian, 620002, Yekaterinburg

I. A. Utepova

Institute of Organic Synthesis named by I.Y. Postovsky, Ural branch of the Russian Academy of Sciences; Ural Federal University named by the first President of Russia B.N. Yeltsin

Email: avs@ios.uran.ru
Russian, 620219, Yekaterinburg; Russian, 620002, Yekaterinburg

A. F. Uglova

Institute of Organic Synthesis named by I.Y. Postovsky, Ural branch of the Russian Academy of Sciences; Ural Federal University named by the first President of Russia B.N. Yeltsin

Email: avs@ios.uran.ru
Russian, 620219, Yekaterinburg; Russian, 620002, Yekaterinburg

O. N. Chupakhin

Institute of Organic Synthesis named by I.Y. Postovsky, Ural branch of the Russian Academy of Sciences; Ural Federal University named by the first President of Russia B.N. Yeltsin

Email: avs@ios.uran.ru
Russian, 620219, Yekaterinburg; Russian, 620002, Yekaterinburg

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Copyright (c) 2023 А.В. Щепочкин, А.Ф. Углова, И.А. Утепова, Е.С. Градоблянская, М.А. Аверков, Н.В. Ковалёва, Е.В. Рудакова, Н.П. Болтнева, О.Г. Серебрякова, Г.Ф. Махаева, В.Н. Чарушин, О.Н. Чупахин