Publication: Synthesis, Anticholinesterase, Antioxidant, and Anti-Aflatoxigenic Activity of Novel Coumarin Carbamate Derivatives
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Date
2018-04-17
Authors
KURT, Belma Zengin
Gazioglu, IŞIL
KANDAS, Nur Ozten
Sonmez, Fatih
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Abstract
New coumarin derivatives with the carbamate moiety were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 4-methyl-2-oxo-2H-chromen-7-yl cycloheptylcarbamate (4h) showed the strongest inhibition against AChE with IC50 values of 2.30 mu M, and 2-oxo-2H-chromen-7-yl-(cyclohexylmethyl)carbamate (4c) and 4-methyl-2-oxo-2H-chromen-7-yl-(cyclohexylmethyl)carbamate (4g) were found to be the most potent BuChE inhibitors with IC50 value of 0.003 mu M and 0.004 mu M, respectively. Moreover antioxidant, anti-aflatoxigenic activities, protective effects against aflatoxin-B1 (AFB1) in H4IIE-C3 cells and effects on glutathione s-transferase of the synthesized compounds were investigated. The synthesized coumarin carbamates inhibited AFB1 in H4IIE-C3 cells. Western blot analyses confirmed that GST alpha protein was induced in cells treated with coumarin carbamates and AFB1. These results showed that the synthesized coumarin carbamates possess a potent protective effect against AFB1.
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KURT B. Z. , Gazioglu I., KANDAS N. O. , Sonmez F., -Synthesis, Anticholinesterase, Antioxidant, and Anti-Aflatoxigenic Activity of Novel Coumarin Carbamate Derivatives-, CHEMISTRYSELECT, cilt.3, ss.3978-3983, 2018