|
ИСТИНА |
Войти в систему Регистрация |
ИПМех РАН |
||
Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitorsстатья
- Авторы: Kobzev M.S., Titov A.A., Alexandrova E.V., Purgatorio R., Catto M., Sorokina E.A., Borisova T.N., Varlamov A.V., Altomare C.D., Voskressensky L.G.
- Журнал: Molecular Diversity
- Том: 26
- Номер: 2
- Год издания: 2022
- Издательство: Springer Nature
- Местоположение издательства: Switzerland
- Первая страница: 1243
- Последняя страница: 1247
- DOI: 10.1007/s11030-021-10185-8
- Аннотация: 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. Graphic abstract: [Figure not available: see fulltext.] © 2021, The Author(s), under exclusive licence to Springer Nature Switzerland AG part of Springer Nature.
- Добавил в систему: Малошицкая Ольга Александровна