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Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones

Author name : OMNIA MAGDY MOHAMMED HENDAWUY
Publication Date : 2018-11-07
Journal Name : Central Nervous System Agents in Medicinal Chemistry

Abstract

(ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer’s dis- ease (AD).
Methods: The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.
Results: Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 μM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.
Conclusion: Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.

Keywords

Acetylcholinesterase, butyrylcholinesterase, chalcone, docking, monoamine oxidase-B, thiophene.

Publication Link

https://doi.org/10.2174/1871524918666181119114016

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