Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones

Parambi DGT 1 , Aljoufi F 2 , Murugaiyah V 3 , Mathew GE 4 , Dev S 5 , Lakshminarayanan B 6 Show all authors , Hendawy OM 2 , Mathew B 6

Affiliations 

  • 1 Department of Pharmaceutical Chemistry, Jouf University, Sakaka, Al Jouf-2014, Saudi Arabia
  • 2 Department of Pharmacology, College of Pharmacy, Al- Jouf University, Sakaka, Al Jouf-2014, Saudi Arabia
  • 3 Discipline of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysia
  • 4 Department of Pharmacology, Grace College of Pharmacy, Palakkad 678004, Kerala, India
  • 5 Department of Pharmaceutical Chemistry, Al Shifa College of Pharmacy, Perinthalmanna 679325, Kerala, India
  • 6 Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala, India
Cent Nerv Syst Agents Med Chem, 2019;19(1):67-71.
PMID: 30451121 DOI: 10.2174/1871524918666181119114016

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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