Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors
| العنوان: | Synthesis of 8-phenyl substituted 3-benzazecines with allene moiety, their thermal rearrangement and evaluation as acetylcholinesterase inhibitors |
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| المؤلفون: | Marco Catto, Rosa Purgatorio, Maxim S. Kobzev, Alexander A. Titov, Elena A. Sorokina, Tatiana N. Borisova, Leonid G. Voskressensky, Elena V. Alexandrova, Alexey V. Varlamov, Cosimo Altomare |
| المصدر: | Molecular Diversity. 26:1243-1247 |
| بيانات النشر: | Springer Science and Business Media LLC, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | 010405 organic chemistry, Chemistry, Stereochemistry, Allene, Organic Chemistry, General Medicine, 010402 general chemistry, 01 natural sciences, Acetylcholinesterase, Catalysis, 0104 chemical sciences, Inorganic Chemistry, chemistry.chemical_compound, Drug Discovery, Moiety, Physical and Theoretical Chemistry, Molecular Biology, Inhibition constant, Derivative (chemistry), Butyrylcholinesterase, Information Systems |
| الوصف: | 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. |
| تدمد: | 1573-501X 1381-1991 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::35648538934a8901057630462084de1e https://doi.org/10.1007/s11030-021-10185-8 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi...........35648538934a8901057630462084de1e |
| قاعدة البيانات: | OpenAIRE |
Find this article in full text from Springer Verlag. | تدمد: | 1573501X 13811991 |
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