Abstract
AbstractNew 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 (4 h) showed the strongest inhibition against AChE with IC50 values of 2.30 μM, and 2‐oxo‐2H‐chromen‐7‐yl‐(cyclohexylmethyl)carbamate (4 c) and 4‐methyl‐2‐oxo‐2H‐chromen‐7‐yl‐(cyclohexylmethyl)carbamate (4 g) were found to be the most potent BuChE inhibitors with IC50 value of 0.003 μM and 0.004 μM, 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 GSTα 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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