N-Phenacylthiazolium Salts as Inhibitors of Cholinesterases

Alla Ocheretniuk, Oleksandr Kobzar, Iryna Mischenko, Andriy Vovk

Abstract


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.


Keywords


acetylcholinesterase; butyrylcholinesterase; thiamin; N-phenacylthiazolium salts; inhibition

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DOI: https://doi.org/10.17721/fujcV5I2P1-14

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