1,2,4-Thiadiazoles as promising multifunctional agents for treatment of neurodegenerative diseases
- Authors: Makhaeva G.F.1, Proshin A.N.1, Boltneva N.P.1, Rudakova E.V.1, Kovaleva N.V.1, Serebryakova O.G.1, Serkov I.V.1, Bachurin S.O.1
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Affiliations:
- Institute of Physiologically Active Compounds, Russian Academy of Sciences
- Issue: Vol 65, No 6 (2016)
- Pages: 1586-1591
- Section: Full Articles
- URL: https://journals.rcsi.science/1066-5285/article/view/238434
- DOI: https://doi.org/10.1007/s11172-016-1486-9
- ID: 238434
Cite item
Abstract
Detailed studies of properties of new 3-substituted 5-anilino-1,2,4-thiadiazoles containing different substituents at position 3 of the thiadiazole ring were carried out, in particular, their esterase profile and antioxidant properties. It was found that the presence in the molecule of 2-aminopropyl fragment determines an efficient and selective inhibition of butyrylcholinesterase as compared to acetylcholinesterase and carboxylesterase, with radical-scavenging activity being weak. The compounds containing a 2-aminopropenyl fragment possess a high radicalscavenging activity, weakly inhibit cholinesterases, and exhibit anticarboxylesterase activity. A wide spectrum of activity of 3-substituted 5-anilino-1,2,4-thiadiazoles as inhibitors of cholinesterases and highly efficient scavengers of free radicals gives a basis for the optimization of structure and development in this series of original agents for therapy of neurodegenerative diseases.
About the authors
G. F. Makhaeva
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
A. N. Proshin
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
N. P. Boltneva
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
E. V. Rudakova
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
N. V. Kovaleva
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
O. G. Serebryakova
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
I. V. Serkov
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432
S. O. Bachurin
Institute of Physiologically Active Compounds, Russian Academy of Sciences
Author for correspondence.
Email: gmakh@ipac.ac.ru
Russian Federation, 1 Severny pr-d, Chernogolovka, Moscow Region, 142432