Imidazole is an azole heterocycle containing two non-adjacent nitrogen atoms added greatly to natural products and synthetic compounds. The planar ring system associated with electronrich nitrogen donors are essential for the greater affinity of imidazole derivatives to bind with various bio receptors and enzymes via weak interactions. It improves the pharmacokinetic properties of the pilot molecules consequently utilized as a solution for aqueous solubility, bioavailability, and toxicity parameters since it is a polar compound. An organic molecule with imidazole derivatives has acquired a sustainable place in medical and clinical fields. The consolidation of the imidazole unit is a significant synthetic technique in drug development.The imidazole-based Schiff bases with enormous therapeutic properties has encouraged the scientists to focus on recently initiated novel chemotherapeutic agents such as anticancer, antimicrobial, antioxidant, antiviral, antileishmanial, etc. Imidazole drugs have expanded the degree of curing different dispositions in clinical medications. Herein, we have reported the structural feature of imidazole, design, synthesis of imidazole derivatives, and its significance. This review aims to describe the reported materials of imidazole-based Schiff bases and their derivatives which offer fruitful scope in the field of medicinal chemistry.