Anticholinesterase and Antioxidant Activity of New Binary Conjugates of γ-Carbolines


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Abstract

The synthesized new binary conjugates of tetrahydro-γ-carbolines, which contained ditriazole spacers of different length, exhibited considerable anticholinesterase and antioxidant activity as well as the potential ability to block the acetylcholinesterase-induced aggregation of β-amyloid in contrast to the original prototype Dimebon. This makes the compounds promising candidates for further investigation as drugs for the treatment of Alzheimer’s disease. Special attention should be given to the conjugate containing the hexamethylene intertriazole spacer, which can be considered as a leader in this series of compounds.

About the authors

G. F. Makhaeva

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Author for correspondence.
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

E. F. Shevtsova

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Author for correspondence.
Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

N. P. Boltneva

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

N. V. Kovaleva

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

E. V. Rudakova

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

L. G. Dubova

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

P. N. Shevtsov

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

S. O. Bachurin

Institute of Physiologically Active Compounds,
Russian Academy of Sciences

Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow oblast, 142432

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