α-Glucosidase is a key enzyme in hydrolysis of carbohydrates to glucose and located in the small in- testine brush border. Inhibition of this enzyme delay the release of glucose and therefore α-glucosidase inhibitors are considered as attractive drugs for treatment of diabetes as a carbohydrate-related disor- der. Due to the importance of α-glucosidase inhibitors in the treatment of diabetes, the discovery and development of new safe and efficient inhibitors for α-glucosidase is an attractive topic for medicinal chemists. In the last decade, 1,2,3-triazole-based derivatives have found much interest in this research field. The click reaction is the most potent tool for easy construction for synthesis of hybrid molecules of 1,2,3-triazole ring and other effective pharmacophors in α-glucosidase inhibition. Herein, an overview is reported on synthesis, biological evaluations, and structure-activity relationships of the reported α- glucosidase inhibitors containing 1,2,3-triazole ring.
