Synthesis and Evaluation of Chalcone and its Derivatives as Potential Anticholinergic Agents

Author(s): Shahzad Murtaza*, Khoula Zubair Mir, Adina Tatheer, Raja Summe Ullah.

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 3 , 2019

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Graphical Abstract:


Background: Structural similarity in Chalcone and Pyrazoline brought our intention for the analysis of such compounds. This study involved the synthesis of chalcones and their pyrazoline derivatives and their screening as cholinesterase inhibitors. The newly synthesized compounds were also investigated for their antioxidant potential.

Methods: Chalcones were synthesized by well-established methods of synthesis and their structural elucidation was carried out by H-NMR, 13C-NMR, Mass spectrometry and FTIR. For the determination of inhibition potency of synthesized compounds, spectrophotometric method was applied whereas, DPPH free radical scavenging method was used to check the antioxidant ability.

Results: Chalcones and their pyrazoline derivatives were synthesized and characterised by 1HNMR, 13C-NMR, Mass spectrometry and FTIR. The compounds were screened for their anti- Alzheimer activity, which exhibited that compounds 1g, 1c and 1h, 1g showed strong inhibitory potency against acetylcholinesterase and butyrylcholinesterase, respectively. DPPH radical scavenging method was applied to check anti-oxidant potential of synthesized compounds and results explored that among all the synthesized compounds only compounds 1c and 1b showed strong scavenging potential.

Conclusion: Chalcone and their pyrazoline derivatives were synthesized and screened for their anti-Alzheimer and antioxidant potential. The experimental results of anti-Alzheimer activity were compared with molecular docking studies, which showed that compounds 1g, 1c and 1h, 1g were active against AChE and BChE, respectively. Among the synthesized compounds 1c and 1b were found to be most potent antioxidants. These results suggest that compound 1b, 1c, 1g and 1h may further be explored for further developments.

Keywords: Antioxidant, chalcone, cholinesterase inhibition, molecular docking, pyrazoline, structure activity relationship.

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Article Details

Year: 2019
Page: [322 - 332]
Pages: 11
DOI: 10.2174/1570180815666180523085436
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