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Aminoadamantane conjugates with carbazole derivatives as potential multitarget agents for the treatment of Alzheimer’s disease. Effect of the spacer structure
- Source :
- Russian Chemical Bulletin. 67:2121-2126
- Publication Year :
- 2018
- Publisher :
- Springer Science and Business Media LLC, 2018.
-
Abstract
- The paper considers the influence of the structure of aminoadamantane–carbazole conjugates linked by five different spacers on their ability to inhibit acetylcholinesterase, butyrylcholinesterase (BChE), and carboxylesterase, the radical scavenging and mitoprotective activity, and tubulin polymerization. The nature of the spacer was found to be determinant for the appearance of anti-BChE and radical-scavenging activity. Aminoadamantane–carbazole conjugates linked by flexible spacers proved to be most effective in these assays. The influence of the conjugates on mitochondrial functions and tubulin polymerization largely depends on the structure of the carbazole moiety. A series of lead compounds promising for further study was identified as potential drugs for the treatment of neurodegenerative diseases, in particular, Alzheimer’s disease.
- Subjects :
- 010405 organic chemistry
Carbazole
General Chemistry
01 natural sciences
Acetylcholinesterase
Combinatorial chemistry
0104 chemical sciences
03 medical and health sciences
chemistry.chemical_compound
Carboxylesterase
0302 clinical medicine
chemistry
Moiety
Tubulin polymerization
030217 neurology & neurosurgery
Butyrylcholinesterase
Conjugate
Subjects
Details
- ISSN :
- 15739171 and 10665285
- Volume :
- 67
- Database :
- OpenAIRE
- Journal :
- Russian Chemical Bulletin
- Accession number :
- edsair.doi...........d78fa2fa13e188e1d6eb9e1c8e57a831
- Full Text :
- https://doi.org/10.1007/s11172-018-2338-6