Email this article Аnticholinesterase and antioxidant activity of new binary conjugates of (с)-carbolines
- Authors: Makhaeva G.F.1, Shevtsova E.F.1, Boltneva N.P.1, Kovaleva N.V.1, Rudakova E.V.1, Dubova L.G.1, Shevtsov P.N.1, Bachurin S.O.1
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Affiliations:
- Institute of Physiologically Active Substances of the Russian Academy of Sciences
- Issue: Vol 484, No 1 (2019)
- Pages: 104-108
- Section: Biochemistry, biophysics, molecular biology
- URL: https://journals.eco-vector.com/0869-5652/article/view/12152
- DOI: https://doi.org/10.31857/S0869-56524841104-108
- ID: 12152
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Abstract
This study presents the synthesis of binary tetrohydro-γ-carbolines with ditriazol spacers of varying length, which exhibit anticholinesterase and antioxidant activity, as compared to the original Dimebon prototype. Anticholinesterase activity suggests the potential ability of the new compounds to block β-amyloid aggregation induced by anticholinesterase, making them promising candidates for further research preparations for the treatment of Alzheimer's disease. Particular attention should be paid to the conjugate with an intertriazol hexamethylene spacer, which can be regarded as the leading compound in this series.
About the authors
G. F. Makhaeva
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Author for correspondence.
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
E. F. Shevtsova
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: shevtsova@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
N. P. Boltneva
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
N. V. Kovaleva
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
E. V. Rudakova
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
L. G. Dubova
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
P. N. Shevtsov
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
Russian Federation, Chernogolovka, Moscow Region, 142432
S. O. Bachurin
Institute of Physiologically Active Substances of the Russian Academy of Sciences
Email: gmakh@ipac.ac.ru
член-корреспондент РАН
Russian Federation, Chernogolovka, Moscow Region, 142432References
- Ustyugov A., Shevtsova E., Bachurin S. // Mol. Neurobiol. 2015. V. 52. № 2. P. 970–978.
- Doody R. S., Gavrilova S. I., Sano M., Thomas R. G., Aisen P. S., Bachurin S. O., Seely L., Hung D. // Lancet. 2008. V. 372. № 9634. P. 207–215.
- Bharadwaj P. R., Bates K. A., Porter T., Teimouri E., Perry G., Steele J. W., Gandy S., Groth D., Martins R. N., Verdile G. // Trans. Psychiatry. 2013. V. 3. P. e332.
- Bachurin S., Bukatina E., Lermontova N., Tkachenko S., Afanasiev A., Grigoriev V., Grigorieva I., Ivanov Y. U., Sablin S., Zefirov N. // Ann. N. Y. Acad. Sci. 2006. V. 939. № 1. P. 425—435.
- Lane R. M., Potkin S. G., Enz A. // Int. J. Neuropsycho-pharmacol. 2006. V. 9. № 1. P. 101–124.
- Inestrosa N. C., Dinamarca M. C., Alvarez A. // FEBS J. 2008. V. 275. № 4. P. 625–632.
- Rosini M., Simoni E., Bartolini M., Soriano E., Marco-Contelles J., Andrisano V., Monti B., Windisch M., Hutter-Paier B., Mcclymont D. W., Mellor I. R., Bolognesi M. L. // ChemMedChem. 2013. V. 8. № 8. P. 1276–1281.
- Соколов В. Б., Аксиненко А. Ю., Горева Т. В., Епишина Т. А., Самсонова А.Н. // ЖОХ. 2018. Т. 88. № 6. С. 1266–1269.
- Makhaeva G. F., Sokolov V. B., Shevtsova E. F., Kovaleva N. V., Lushchekina S. V., Boltneva N. P., Rudakova E. V., Aksinenko A. Y., Shevtsov P. N., Neganova M. E., Dubova L. G., Bachurin S. O. // Pure and Appl. Chem. 2017. V. 89. № 8. P. 1167—1184.
- Hatfield M. J., Potter P. M. // Expert Opin. Ther. Pat. 2011. V. 21. № 8. P. 1159–1171.
- Makhaeva G. F., Lushchekina S. V., Boltneva N. P., Serebryakova O. G., Rudakova E. V., Ustyugov A. A., Bachurin S. O., Shchepochkin A. V., Chupakhin O. N., Charushin V. N., Richardson R. J. // Bioorg. Med. Chem. 2017. V. 25. № 21. P. 5981–5994.
- Taylor P., Lappi S. // Biochemistry. 1975. V. 14. № 9. P. 1989–1997.
- Moreira P. I., Siedlak S. L., Aliev G., Zhu X., Cash A. D., Smith M. A., Perry G. // J. Neural. Trans. 2005. V. 112. № 7. P. 921–932.
- Wilbur K. M. B. F., Shapiro O. W. // Arch. Biochem. 1949. V. 24. № 2. P. 305–313.
- Re R., Pellegrini N., Proteggente A., Pannala A., Yang M., Rice-Evans C. // Free Radic. Biol. Med. 1999. V. 26. № 9/10. P. 1231–1237.
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