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RESEARCH ARTICLE
Year : 2017  |  Volume : 6  |  Issue : 2  |  Page : 134-141

Synthesis, docking and acetylcholinesterase inhibitory evaluation of (E)-3-(4-(diethylamino) phenyl)-1-phenylprop-2-en-1-one derivatives with probable anti-Alzheimer effects


1 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
2 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Pharmacology, Toxicology and Medical Services, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
3 Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences; Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran
4 Isfahan Pharmaceutical Sciences Research Center, Isfahan, Iran

Correspondence Address:
Alireza Aliabadi
Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah
Iran
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Source of Support: None, Conflict of Interest: None


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Alzheimer's disease (AD) as form of senile dementia is a cognitive and neurodegenerative disorder as well as behavioral and psychological problems in the geriatric people. The disease is characterized by memory deficit as well as decline in daily activities. The deficiency of the cholinergic system is one the main causes of the disease. Some medications such as donepezil are capable of enhancement of the acetylcholine neurotransmitter via the inhibition of the acetylcholinesterase (AChE) enzyme. According to the positive background of the chalcone derivatives in inhibition of AChE, a new series of chalcone derivatives were synthesized using aldol condensation procedure and their enzyme inhibitory potency were assessed by Ellman's test. Some of the tested derivatives demonstrated superior activity than donepezil (IC50 = 0.41 ± 0.09 μM) especially methoxylated compounds 3h (2-OCH3, IC50 = 0.1 ± 0.02 μM), 3i (3-OCH3, IC50 = 0.12 ± 0.03 μM) and 3j (4-OCH3, IC50 = 0.39 ± 0.04 μM). Compound 3b (3-Cl, IC50 = 0.13 ± 0.03 μM) also possessed higher activity than donepezil. Molecular docking investigation also confirmed an effective hydrogen bonding interaction of 3h with AChE. In conclusion, the synthesized compounds could be suggested as new anti-acetylcholinesterase lead compounds.


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