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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Published in | French-Ukrainian journal of chemistry Vol. 5; no. 2; pp. 1 - 14 |
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Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
2017
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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. |
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AbstractList | 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. |
Author | Mischenko, Iryna Vovk, Andriy Ocheretniuk, Alla Kobzar, Oleksandr |
Author_xml | – sequence: 1 givenname: Alla surname: Ocheretniuk fullname: Ocheretniuk, Alla organization: Institute of Bioorganic Chemistry and Petrochemistry of National Academy of Sciences of Ukraine – sequence: 2 givenname: Oleksandr surname: Kobzar fullname: Kobzar, Oleksandr organization: Institute of Bioorganic Chemistry and Petrochemistry of National Academy of Sciences of Ukraine – sequence: 3 givenname: Iryna surname: Mischenko fullname: Mischenko, Iryna organization: Institute of Bioorganic Chemistry and Petrochemistry of National Academy of Sciences of Ukraine – sequence: 4 givenname: Andriy surname: Vovk fullname: Vovk, Andriy organization: Institute of Bioorganic Chemistry and Petrochemistry of National Academy of Sciences of Ukraine |
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