Schiff bases represent an important class of organic compounds owing to their wide range of biological activities and industrial applications. They are characterized by the presence of azomethine group and formed by the condensation of primary amines with aldehydes or ketones. They also serve as a back bone for the synthesis of various heterocyclic compounds. Since last few decades, a variety of Schiff bases and their derivatives have been synthesized and reported to possess a wide variety of biological activities i.e. anticancer, antioxidant, antiglycation, antimicrobial, antimalarial, antiviral and CNS activities. This review highlights the synthetic strategies of novel Schiff bases of different heterocycles and their evaluation for different CNS activities.