Schiff bases are the condensation products of primary amines and carbonyl compounds, which are becoming more and more significant. Schiff bases are imine or azomethine (–C=N–) functional group containing compounds that are produced through a nucleophile addition process. Excellent chelators called Schiff bases have a place in both qualitative and quantitative analysis of metals in aqueous media. Schiff bases were discovered to be auxiliary scaffolds and adaptable pharmacophore for the creation and production of numerous bioactive leads compounds, and this special quality made them accessible for a wide range of biological applications. Schiff bases exhibit significant biological properties including analgesic, anti-inflammatory, antibacterial, anticonvulsant, anti-tubercular, anticancer, antioxidant, anthelmintic antiglycation, and antidepressant activities. In situ cross-linked hydrogel systems are created using the Schiff bases, which are frequently utilized in coordination, organometallic chemistry, and tissue engineering applications. The role of Schiff bases to the design and creation of new lead with potential biological functions is highlighted in this chapter. Researchers’ interest in obtaining the most conclusive and suggestive information on the numerous Schiff bases that have been important for therapeutic purposes over the last few decades and their use in coordination complexes has been maintained by this bioactive core.