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ЖУРНАЛЫ // Mendeleev Communications // Архив

Mendeleev Commun., 2023, том 33, выпуск 1, страницы 77–79 (Mi mendc313)

Эта публикация цитируется в 5 статьях

Communications

Annulated bicyclic isothioureas: identification of active and selective butyrylcholinesterase inhibitors

E. V. Nurievaa, A. A. Alexeeva, N. A. Zefirovab, E. R. Milaevaab, N. V. Kovalevab, A. N. Proshinb, G. F. Makhaevab, O. N. Zefirovaab

a Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
b Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation


Аннотация: Structural optimization of butyrylcholinesterase inhibitors, 5-bromomethyl- and 5-iodomethyl-N,N-disubstituted 2-aminothiazolines, led to a series of their annulated bicyclic analogues, obtained by intramolecular cyclization of cycloalkenylthioureas. The most active compound in this series, cyclohepta[d]thiazol-2-amine, is a mixed-type butyryl-cholinesterase inhibitor with IC50 = 130 nm, highly selective compared to acetylcholinesterase and non-toxic at 100 μm concentrations.

Ключевые слова: bicyclic isothioureas, cycloalka[d]thiazole-2-amine, thioureas, 2-aminothiazolines, heterocyclization, butyrylcholinesterase inhibitors, Alzheimer’s disease, cytotoxicity.

Язык публикации: английский

DOI: 10.1016/j.mencom.2023.01.024



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