ACETYLCHOLINESTERASE INHIBITORY EFFECT OF 3-(1H-INDOL-3-YL)-1, 3-DIPHENYLPROPAN-1-ONE DERIVATIVES


Manjunatha K S, Manu Cp, Satyanarayan Nd, Vinay Kn, Vineetha Ms, Sunil More S

Abstract


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.


Keywords


Alzheimer’s disease, Neurotransmitter, Dementia, Bovine serum albumin, Ellman’s method, Physostigmine.

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About this article

Title

ACETYLCHOLINESTERASE INHIBITORY EFFECT OF 3-(1H-INDOL-3-YL)-1, 3-DIPHENYLPROPAN-1-ONE DERIVATIVES

Keywords

Alzheimer’s disease, Neurotransmitter, Dementia, Bovine serum albumin, Ellman’s method, Physostigmine.

DOI

10.22159/ajpcr.2017.v10i8.18730

Date

01-08-2017

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 10 Issue 8 August 2017 Page: 83-86

Print ISSN

0974-2441

Online ISSN

2455-3891

Statistics

51 Views | 94 Downloads

Authors & Affiliations

Manjunatha K S
Department of Pharmaceutical Chemistry, Kuvempu University, Post Graduate Centre, Kadur - 577 548, Chikkamagalur, Karnataka, India.
India

Manu Cp
Department of Pharmaceutical Chemistry, Kuvempu University, Post Graduate Centre, Kadur - 577 548, Chikkamagalur, Karnataka, India.
India

Satyanarayan Nd
Department of Pharmaceutical Chemistry, Kuvempu University, Post Graduate Centre, Kadur - 577 548, Chikkamagalur, Karnataka, India.
India

Vinay Kn
Department of Chemistry, Tumkur University, Tumkur - 572 101, Karnataka, India
India

Vineetha Ms
Department of Biochemistry, Centre for Post Graduate Studies, Jain University, Bengaluru, Karnataka, India.
India

Sunil More S
School of Basic and Applied Sciences, Dayananda Sagar University, K.S. Layout, SM Hills, Bengaluru - 560 078, Karnataka, India
India


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