Coumarin-based Scaffold as α-glucosidase Inhibitory Activity: Implication for the Development of Potent Antidiabetic Agents.

Background: Delaying the absorption of glucose through α-glucosidase enzyme inhibition is one of the therapeutic approaches in the management of Type 2 diabetes, which can reduce the incidence of postprandial hyperglycemia. The existence of chronic postprandial hyperglycemia impaired the endogenous antioxidant defense by inducing oxidative stress-induced pancreatic β-cell destruction through uncontrolled generation of free radicals such as ROS, which in turn, leads to various macrovascular and microvascular complications. The currently available α -glucosidase inhibitors, for instance, acarbose, have some side effects such as hypoglycemia at higher doses, liver problems, meteorism, diarrhea, and lactic acidosis. Therefore, there is an urgent need to discover and develop potential α-glucosidase inhibitors.

Objective: Based on suchmotifs, researchers are intrigued to search for the best scaffold that displays various biological activities. Among them, coumarin scaffold has attracted great attention. The compound and its derivatives can be isolated from various natural products and/or synthesized for the development of novel α-glucosidase inhibitors.

Results: This study focused on coumarin and its derivatives as well as on their application as potent antidiabetic agents and has also concentrated on the structure-activity relationship.

Conclusion: This review describes the applications of coumarin-containing derivatives as α - glucosidase inhibitors based on published reports which will be useful for innovative approaches in the search for novel coumarin-based antidiabetic drugs with less toxicity and more potency.