Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.

Cent Nerv Syst Agents Med Chem

Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala, India.

Published: November 2019

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.

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Source
http://dx.doi.org/10.2174/1871524918666181119114016DOI Listing

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