Recent Advances of α-Glucosidase Inhibitors: A Comprehensive Review

Background: Diabetes mellitus (DM) is a critical health issue prevailing in nearly half a billion people worldwide. It is one of the most threatening metabolic diseases. Type 2 DM is caused due to insulin resistance and accounts for 90% of diabetes cases. If it remains untreated, it can lead to major frightening complications and can cause death, which ultimately threatens humankind. Discussion: Various oral hypoglycaemic drugs are available today, acting on different targets by adopting different pathways. However, the alpha-glucosidase inhibitors proved to be a novel and effective strategy to manage T2DM. These inhibitors alleviate postprandial glycemia by aiming to inhibit intestinal alpha-glucosidase competitively and reversibly, thus delaying carbohydrate digestion and turning down the rate of glucose absorption. Plenty of alpha-glucosidase inhibitors have been discovered from synthetic routes as well as from natural sources, including plants, fungi, and bacteria. Conclusion: This article comprises the natural and synthetic alpha-glucosidase discovered from 2016 to 2021 and can be utilized to discover novel alpha-glucosidase inhibitors. This review is an endeavor to highlight the progress in the discovery and development of alpha-glucosidase inhibitors, which could provide an overview to the medicinal chemists for the development of clinically viable drugs using this information.