ACETYLCHOLINESTERASE INHIBITORY EFFECT OF 3-(1H-INDOL-3-YL)-1, 3-DIPHENYLPROPAN-1-ONE DERIVATIVES
DOI:
https://doi.org/10.22159/ajpcr.2017.v10i8.18730Keywords:
Nil, Neurotransmitter, Dementia, Bovine serum albumin, Nil, PhysostigmineAbstract
Objective: The objective of the study is acetylcholinesterase (AChE) inhibitory effect of 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives by Ellman's method, physostigmine is used as positive control.
Method: 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were synthesized by the addition of chalcone (0.25 g, 1 mmol), indole (0.12 g, 1 mmol) in ethanol (5 ml), and concentrated hydrochloric acid (5 mmol %). These earlier synthesized compounds were screened for AChE inhibitors by modifying Ellman's method.
Results: Among the tested compounds, 3a and 3j were found to be having more potential than other compounds with half maximal inhibitory concentration values of 13.64 and 14.3 μg/ml, respectively. Whereas, compounds 3c, 3e, 3g, and 3i exhibited an average AChE inhibition of 16.4, 17.9, 17.6, and 21.1 μg/ml, respectively.
Conclusion: The compounds 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were found to be possible lead molecules in AChE inhibition and even though, the molecules were structurally dissimilar to that of the standard, still they exhibited a considerable degree of inhibition and encourage the researchers to look into the mode of action of their inhibition ability against AChE.
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