The search for metal-derived antioxidants has received much attention and effort in order to identify the compounds having high capacity in scavenging free radicals related to various disorders and diseases associated with oxidative damage, caused by reactive oxygen species (ROS). Presently, synthetic antioxidants are widely used because they are effective and cheaper than natural antioxidants. Currently a number of Schiff-base metal complexes have been investigated as effective scavengers of ROS, acting as antioxidants. The aim of this review is to highlight specific characteristics of Schiff-based compounds capable of chelating metal ions and their antioxidant activity. Schiff bases form an important class of organic compounds with a wide variety of biological properties. Schiff bases have often been used as chelating ligands in the field of coordination chemistry, and their metal complexes have been of great interest to researchers for many years. The activity is usually increased by complexation therefore to understand the properties of both ligands and metal can lead to the synthesis of highly active compounds. The influence of certain metals on the biological activity of these compounds and their intrinsic chemical interest as multidentate ligands has prompted a considerable increase in the study of their coordination behavior. Development of a new chemotherapeutic Schiff bases and their metal complexes is now attracting the attention of medicinal chemists.