N-Phenacylthiazolium Salts as Inhibitors of Cholinesterases

Inhibition of acetylcholinesterase is considered as a promising approach for treatment of neurodegenerative disorders including Alzheimer's disease. In this study, we demonstrated that 5-substituted N-phenacylthiazolium derivatives are capable of inhibiting acetylcholinesterase and butyrylcholi...

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Bibliographic Details
Published inFrench-Ukrainian journal of chemistry Vol. 5; no. 2; pp. 1 - 14
Main Authors Ocheretniuk, Alla, Kobzar, Oleksandr, Mischenko, Iryna, Vovk, Andriy
Format Journal Article
LanguageEnglish
Published 2017
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Summary:Inhibition of acetylcholinesterase is considered as a promising approach for treatment of neurodegenerative disorders including Alzheimer's disease. In this study, we demonstrated that 5-substituted N-phenacylthiazolium derivatives are capable of inhibiting acetylcholinesterase and butyrylcholinesterase activities with IC50 values in the micromolar range. Some of the new thiazolium-based inhibitiors showed more than 10-fold selectivity for butyrylcholinesterase. Kinetic experiments and molecular docking were performed for understanding the inhibition mechanisms.
ISSN:2312-3222
2312-3222
DOI:10.17721/fujcV5I2P1-14