•Recent developments in synthetic α-glucosidase inhibitors.•Structure activity relationship.•Molecular modeling studies.•Future perspective for development of potent and safer α-glucosidase inhibitors discussed. Diabetes mellitus is the prominent metabolic disorder affecting 422 million people around the globe and cause severe associated problems like kidney disorders, heart and nervous system diseases, leg amputation and retinopathy. Currently marketed antidiabetic drugs are failing in containment of this disorder that arise a need for novel and potent antidiabetic agents. α-Glucosidase provide a viable target to tackle this disorder and attracted significant attention of medicinal chemists globally. Recent literature reports revealed improved therapeutic potential of α-glucosidase inhibitors due to their synergistic potency, better safety and competitive type of inhibition. Medicinal chemists have gone to great extents for the design of novel α-glucosidase inhibitors by generating structural hybrids of different key molecules, heterocycles with improved binding affinities and potency towards the enzyme. This article summarized recently published α-glucosidase inhibitors as potential antidiabetic agents. Their pharmacological outputs, structural-activity relationships, mechanistic and in silico studies are well analyzed. This article will be highly useful for the researchers working in this filed to design and develop novel and potent α-glucosidase inhibitors as potential antidiabetic agents with improve potency and therapeutic efficacy. Display omitted