Diabetes mellitus is a chronic metabolic disease which is characterized by high blood sugar levels over a prolonged period of time. Uncontrolled hyperglycemia can lead to serious damage to many vital organs in the body, including kidney damage, heart disease, and nerve damage. The goal of treatment of diabetes mellitus is reduction of blood glucose levels and controlling subsequent complications. Different mechanisms are involved in diabetes mellitus treatment. Quinazolinone and its derivatives have been found as effective and versatile pharmacophoric units in medicinal chemistry to design and develop a wide range of bioactive compounds.   The present review summarizes the advances in lead compounds of quinazolinone hybrids and their related heterocycles in treatment of diabetes mellitus. Moreover, the review also helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features in exhibiting the hypoglycemic effect. Keywords: Quinazolinone, Diabetes mellitus, Drug design, Antidiabetic