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Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.

Publication Type : Journal Article

Publisher : Cent Nerv Syst Agents Med Chem

Source : Cent Nerv Syst Agents Med Chem, Volume 19, Issue 1, p.67-71 (2019)

Keywords : acetylcholinesterase, Animals, Chalcones, Cholinesterase Inhibitors, Crystallography, X-Ray, Horses, Humans, Monoamine oxidase, Monoamine Oxidase Inhibitors, Structure-Activity Relationship

Campus : Kochi

School : School of Pharmacy

Department : Pharmaceutical Chemistry & Analysis

Year : 2019

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.

Cite this Research Publication : D. G. T. Parambi, Aljoufi, F., Murugaiyah, V., Mathew, G. E., Dev, S., Lakshminarayanan, B., Hendawy, O. M., and Bijo Mathew, “Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.”, Cent Nerv Syst Agents Med Chem, vol. 19, no. 1, pp. 67-71, 2019.

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