Synthetic α-glucosidase inhibitors as promising anti-diabetic agents: Recent developments and future challenges

Eur J Med Chem. 2023 Mar 5;249:115119. doi: 10.1016/j.ejmech.2023.115119. Epub 2023 Jan 17.


Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st century. It is a well-recognized multifactorial health problem contributes significantly to high mortality rates by causing serious health complications mainly related to cardiovascular diseases, kidney damage and neuropathy. The inhibition of α-glucosidase (enzyme that catalyses starch hydrolysis in the intestine) is an effective therapeutic approach for controlling hyperglycemia associated with type-2 diabetes. However, the presently approved drugs/inhibitors such as acarbose, miglitol and voglibose have several undesirable gastrointestinal side effects impeding their applications. Therefore, search for novel and more effective inhibitors with reduced side effects and less cost remains a fascinating area of research. In this context, a large variety of α-glucosidase inhibitors have been identified in recent years that demands attention from drug development community. This review is therefore an effort to summarize and highlight the promising α-glucosidase inhibitors especially those which are primarily based on aromatic heterocyclic scaffolds such as coumarin, imidazole, isatin, pyrimidine, quinazoline, triazine, thiazole etc, having improved safety and pharmacological profiles.

Keywords: Diabetes mellitus; Heterocyclic; Structure-activity relationship (SAR); Synthetic; α-Glucosidase inhibitors.

Publication types

  • Review

MeSH terms

  • Acarbose / pharmacology
  • Acarbose / therapeutic use
  • Diabetes Mellitus, Type 2* / drug therapy
  • Glycoside Hydrolase Inhibitors* / pharmacology
  • Glycoside Hydrolase Inhibitors* / therapeutic use
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Hypoglycemic Agents / therapeutic use
  • alpha-Glucosidases


  • Glycoside Hydrolase Inhibitors
  • Hypoglycemic Agents
  • Acarbose
  • alpha-Glucosidases