The urease enzyme, found in plants, fungi and bacteria, plays a crucial role in catalyzing the hydrolysis of urea, a process integral to microbial metabolism. Its ureolytic activities have garnered significant attention for their impact on agriculture and the health of living organisms. Notably, urease activity in the human stomach, urinary tract and animal cells can lead to pathogenic outcomes. Schiff bases, characterized by their carbonyl-type imine or azomethine linkage, are recognized for their diverse biological effects, including anti-urease activity. Additionally, the metal complexes derived from the Schiff bases demonstrate controlled urease inhibition activity, influenced by factors such as the type of metal, its oxidation state and the coordination environment. This inhibition occurs through the interaction of the Schiff base ligand with the nickel containing active site of urease or the protein sphere surrounding the metal, disrupting the ureolytic mechanism. In this review, the utilization of Schiff bases and their metal complexes in urease inhibition is highlighted as explored by various research groups.