Biological Studies of Novel Aspirin-Chalcone Derivatives bearing Variable Substituents
The evolution of drug resistant bacteria has now becoming a major concern in the search for new antibacterial agent. Ongoing interest has also developing to find a new class of compounds with antioxidant properties. Herein, a series of hydroxylated chalcones 1a-g and aspirin-chalcone...
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| Main Authors: | , , |
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| Format: | Article |
| Language: | en |
| Published: |
Penerbit Universiti Sultan Zainal Abidin
2020
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| Subjects: | |
| Online Access: | http://ir.unimas.my/id/eprint/34093/1/Biological%20Studies%20of%20Novel%20Aspirin-Chalcone%20Derivatives%20bearing%20Variable%20Substituents.pdf http://ir.unimas.my/id/eprint/34093/ https://journal.unisza.edu.my/agrobiotechnology/index.php/agrobiotechnology/index |
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| Summary: | The evolution of drug resistant bacteria has now becoming a major concern in the search for new antibacterial agent. Ongoing interest has also developing to find a new class of compounds with antioxidant properties. Herein, a series of hydroxylated chalcones 1a-g and aspirin-chalcone derivatives 2a-g were successfully synthesised for antibacterial and antioxidant properties. Chalcones 1a-g were prepared by Claisen-Schmidt condensation of 4-hydroxyacetophenone and benzaldehyde derivatives, while 2a-g were synthesised viaesterification of aspirin with 1a-g. All the synthesised compounds were elucidated using CHNS elemental analysis, FTIR, 1H and 13C NMR spectroscopy, and X-ray crystallography. All compounds were evaluated for antibacterial assay via disc diffusion method and antioxidant assay using stable free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH). Only 1ashowed moderate activity against Escherichia coli, while 1b-gand 2a-gshowed no inhibition against E. coliand Staphylococcus aureusin comparison ampicillin as standard antibiotic. Compounds 1b-g and 2a-g having various substituents contributed to bulky molecular structures and caused difficult penetration into the cell membrane thus, unable to inhibit the bacterial growth. Compounds 1a-gand 2a-g also displayed poor antioxidant properties on DPPH in comparison to ascorbic acid due to low phenolic pharmacophore. The formation of bulky structures for 2a-g have hindered the antioxidant properties compared to 1a-g. |
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