Submit Manuscript  

Article Details


Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones

[ Vol. 19 , Issue. 1 ]

Author(s):

Della G.T. Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa E. Mathew, Sanal Dev, Balasubramanain Lakshminarayanan, Omnia M. Hendawy and Bijo Mathew*   Pages 67 - 71 ( 5 )

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.

Affiliation:

Department of Pharmaceutical Chemistry, Jouf University, Sakaka, Al Jouf-2014, Department of Pharmacology, College of Pharmacy, Al- Jouf University, Sakaka, Al Jouf-2014, Discipline of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Penang, Department of Pharmacology, Grace College of Pharmacy, Palakkad 678004, Kerala, Department of Pharmaceutical Chemistry, Al Shifa College of Pharmacy, Perinthalmanna 679325, Kerala, Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala, Department of Pharmacology, College of Pharmacy, Al- Jouf University, Sakaka, Al Jouf-2014, Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala

Graphical Abstract:



Read Full-Text article