Miglitol

Gut microbiota act as beneficial symbionts of the hosts. Administration of α-glucosidase inhibitors (α-GIs) is considered to promote the microbiota's carbohydrate availability, modulating short-chain fatty acid (SCFA) production. However, it remains unclear whether host-microbiota interaction differs depending on α-GI types (e.g., acarbose versus miglitol) and carbohydrate types co-administered. In this study, we demonstrate that acarbose is transported through bacterial outer membrane porins, LamB and ScrY, and inhibits maltose metabolism in Escherichia coli. Furthermore, studies using Klebsiella pneumoniae reveal that acarbose suppresses utilization of maltose, but not that of sucrose. When co-administered with acarbose in mice, sucrose, relative to maltose, enhances SCFA production, suppresses glucose-dependent insulinotropic polypeptide (GIP) secretion, and protects against high-fat diet-induced obesity, underscoring the importance of sucrose as a microbiota-dependent beneficial factor, but not a culprit in host metabolism. In conclusion, acarbose regulates host metabolic processes partly by modulating gut microbial metabolism in a carbohydrate-type-dependent manner.

Type 2 diabetes mellitus (T2DM) poses a widespread challenge to public health across the globe, necessitating the development of safer and more effective therapeutic agents. α- glucosidase has emerged as an important therapeutic target due to its role in delaying carbohydrate digestion and controlling postprandial glucose levels; its inhibition slows glucose absorption in the small intestine, effectively helping to manage postprandial hyperglycemia. Existing α-glucosidase inhibitors such as acarbose, miglitol, and voglibose are constrained by gastrointestinal side effects and limited efficacy. These drawbacks, along with complex synthesis, have directed current research toward designing simpler heterocyclic scaffolds as potential α-glucosidase inhibitors. Click chemistry offers a versatile and efficient synthetic approach based on simple, reliable reactions. Recent advances in medicinal chemistry highlight 1,2,3-triazole scaffolds derived from click chemistry as promising frameworks for designing novel α-glucosidase inhibitors with enhanced bioactivity. This review evaluates 1,2,3-triazole-based compounds developed between 2019 and 2025 for their inhibitory potential. A wide spectrum of triazole-linked hybrids, including quinoline, coumarin, xanthone, and benzimidazole, is examined with a focus on their synthesis, in vitro potency, and structureactivity relationship analyses. The findings emphasize how specific substituents, such as halogen and electron-withdrawing groups, could modulate biological activity. Furthermore, challenges in development, including protein/receptor specificity, synthetic complexity, and side effects of α- glucosidase inhibitors, are discussed alongside future directions for the rational design of more efficacious and target-specific inhibitors. This work consolidates recent progress and underscores the potential of 1,2,3-triazole derivatives as an effective motif in the ongoing quest for improvement of antidiabetic therapeutics.