Title
Novel conjugates of aminoadamantanes with carbazole derivatives as potential multitarget agents for AD treatment
Date Issued
30 March 2017
Access level
open access
Resource Type
journal article
Author(s)
Bachurin S.
Shevtsova E.
Makhaeva G.
Grigoriev V.
Boltneva N.
Kovaleva N.
Lushchekina S.
Shevtsov P.
Neganova M.
Redkozubova O.
Bovina E.
Gabrelyan A.
Fisenko V.
Sokolov V.
Aksinenko A.
Echeverria V.
Aliev G.
Universidad Autónoma de Chile
Publisher(s)
Nature Publishing Group
Abstract
A new group of compounds, promising for the design of original multitarget therapeutic agents for treating neurodegenerative diseases, based on conjugates of aminoadamantane and carbazole derivatives was synthesized and investigated. Compounds of these series were found to interact with a group of targets that play an important role in the development of this type of diseases. First of all, these compounds selectively inhibit butyrylcholinesterase, block NMDA receptors containing NR2B subunits while maintaining the properties of MK-801 binding site blockers, exert microtubules stabilizing properties, and possess the ability to protect nerve cells from death at the calcium overload conditions. The leading compound C-2h has been shown the most promising effects on all analyzed parameters. Thus, these compounds can be regarded as promising candidates for the design of multi-target disease-modifying drugs for treatment of AD and/or similar neuropathologies.
Volume
7
Language
English
OCDE Knowledge area
Farmacología, Farmacia
Bioquímica, Biología molecular
Scopus EID
2-s2.0-85016644033
PubMed ID
Source
Scientific Reports
ISSN of the container
20452322
Sponsor(s)
The study was supported by the grant of the Russian Science Foundation (project number 14-23-00160). Authors are grateful to the Lomonosov State University Research Super Computer Center for providing computational facilities92.
Sources of information:
Directorio de Producción Científica
Scopus