Annulated bicyclic isothioureas: identification of active and selective butyrylcholinesterase inhibitors

Nurieva E.; Alexeev A.; Zefirov N.; Elena R. Milaeva; Kovaleva N.; Proshin A.; Makhaeva G.; Zefirova O.

doi:10.1016/j.mencom.2023.01.024

Публикации

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Annulated bicyclic isothioureas: identification of active and selective butyrylcholinesterase inhibitors

Mendeleev Communications. 2023. Vol. 33. No. 1. P. 77–79.

Nurieva E., Alexeev A., Zefirov N., Elena R. Milaeva, Kovaleva N., Proshin A., Makhaeva G., Zefirova O.

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 butyrylcholinesterase inhibitor with IC50 = 130 nm, highly selective compared to acetylcholinesterase and non-toxic at 100 mm concentrations.

Научное направление: Химия

Язык: английский

Полный текст

DOI

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

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