Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors
Maxim S Kobzev
1
,
Alexander A Titov
1
,
Elena V Aleksandrova
1
,
Rosa Purgatorio
2
,
Marco Catto
2
,
Elena A Sorokina
1
,
T. Borisova
1
,
Cosimo Altomare
2
,
Publication type: Journal Article
Publication date: 2021-02-04
scimago Q2
wos Q2
SJR: 0.646
CiteScore: 8.5
Impact factor: 3.8
ISSN: 13811991, 1573501X
PubMed ID:
33538985
Catalysis
Organic Chemistry
Drug Discovery
Inorganic Chemistry
Physical and Theoretical Chemistry
Molecular Biology
General Medicine
Information Systems
Abstract
Various 4′-R-substituted phenyl azacyclic allenes were synthesized in good yields, and their thermal transformations were studied. For the first time, the obtained rearrangement products—new N-bridged cyclopenta[a]indenes, and the corresponding parent allenes were evaluated as potential inhibitors of acetyl- and butyrylcholinesterase. Among the tested compounds, the allene derivative 2g proved to competitively inhibit human AChE with inhibition constant value (Ki) in the low micromolar range.
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Total citations:
6
Citations from 2024:
2
(33.33%)
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Kobzev M. S. et al. Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors // Molecular Diversity. 2021. Vol. 26. No. 2. pp. 1243-1247.
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Kobzev M. S., Titov A. A., Aleksandrova E. V., Purgatorio R., Catto M., Sorokina E. A., Borisova T., Varlamov A. V., Altomare C., Voskressensky L. G. Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors // Molecular Diversity. 2021. Vol. 26. No. 2. pp. 1243-1247.
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RIS
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TY - JOUR
DO - 10.1007/s11030-021-10185-8
UR - https://doi.org/10.1007/s11030-021-10185-8
TI - Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors
T2 - Molecular Diversity
AU - Kobzev, Maxim S
AU - Titov, Alexander A
AU - Aleksandrova, Elena V
AU - Purgatorio, Rosa
AU - Catto, Marco
AU - Sorokina, Elena A
AU - Borisova, T.
AU - Varlamov, Alexey V.
AU - Altomare, Cosimo
AU - Voskressensky, Leonid G.
PY - 2021
DA - 2021/02/04
PB - Springer Nature
SP - 1243-1247
IS - 2
VL - 26
PMID - 33538985
SN - 1381-1991
SN - 1573-501X
ER -
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BibTex (up to 50 authors)
Copy
@article{2021_Kobzev,
author = {Maxim S Kobzev and Alexander A Titov and Elena V Aleksandrova and Rosa Purgatorio and Marco Catto and Elena A Sorokina and T. Borisova and Alexey V. Varlamov and Cosimo Altomare and Leonid G. Voskressensky},
title = {Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors},
journal = {Molecular Diversity},
year = {2021},
volume = {26},
publisher = {Springer Nature},
month = {feb},
url = {https://doi.org/10.1007/s11030-021-10185-8},
number = {2},
pages = {1243--1247},
doi = {10.1007/s11030-021-10185-8}
}
Cite this
MLA
Copy
Kobzev, Maxim S., et al. “Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors.” Molecular Diversity, vol. 26, no. 2, Feb. 2021, pp. 1243-1247. https://doi.org/10.1007/s11030-021-10185-8.