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Central Nervous System Agents in Medicinal Chemistry

Author(s): Della G.T. Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa E. Mathew, Sanal Dev, Balasubramanain Lakshminarayanan, Omnia M. Hendawy and Bijo Mathew*

DOI: 10.2174/1871524918666181119114016

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Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones

Page: [67 - 71] Pages: 5

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Abstract

Background: Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer’s disease (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.

Graphical Abstract

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