Novel N‐methylated ebselenamine antioxidants were prepared from their corresponding diselenides with iodomethane. All ebselenamines showed excellent chain‐breaking and glutathione peroxidase (GPx)‐like activities. These could also inhibit the lipid peroxidation much more efficiently than α‐tocopherol. They could also mimic the functions of the GPx enzymes nearly two times better than ebselen in the coupled reductase assay. Also, these were found to scavenge the ROS produced at low concentration (10 μM) with low toxicity effects and would have the therapeutic potential against autoxidation. It is anticipated that these compounds would have the potential to be used in several diseases caused by autoxidation, and thus, providing protection for mammalians from cell death.