Diabetes mellitus is a chronic and most prevalent metabolic disorder affecting 422 million the people worldwide and causing life‐threatening associated conditions including disorders of kidney, heart, and nervous system as well as leg amputation and retinopathy. Steadily rising cases from the last few decades suggest the failure of currently available drugs in containment of this disease. α‐Glucosidase is a potential target for effectively tackling this disease and attracting significant interest from medicinal chemists around the globe. Besides having a set of side effects, currently available α‐glucosidase inhibitors (carbohydrate mimics) offer better tolerability, safety, and synergistic pharmacological outcomes with other antidiabetic drugs therefore medicinal chemists have working extensively over last three decades for developing alternative α‐glucosidase inhibitors. The 1,2,3‐Triazole nucleus is energetically used by various research groups around the globe for the development of α‐glucosidase inhibitors posing it as an optimum scaffold in the field of antidiabetic drug development. This review is a systematic analysis of α‐glucosidase inhibitors developed by employing 1,2,3‐triazole scaffold with special focus on design strategies, structure‐activity relationships, and mechanism of inhibitory effect. This article will act as lantern for medicinal chemists in developing of potent, safer, and effective α‐glucosidase inhibitors with desired properties and improved therapeutic efficacy.