Tehran University of Medical Sciences

Science Communicator Platform

Share By
Recent Advances on the Α-Glucosidase Inhibitory Activity of Benzimidazoles Publisher Pubmed



Shafiee SM ; Asadi M ; Mahdavi M ; Saeedi M
Authors

Source: Archiv der Pharmazie Published:2026


Abstract

Benzimidazole derivatives have emerged as important scaffolds in the development of potent and effective α-glucosidase inhibitors, key targets for managing type 2 diabetes mellitus (T2DM). This review highlights structural innovations and structure–activity relationships (SARs) of diverse benzimidazole-based compounds, including hybrids with Schiff bases, thiosemicarbazones, 1,2,3-triazoles, and oxadiazoles, all exhibiting α-glucosidase inhibitory activity. Notably, numerous derivatives demonstrate superior inhibition compared to the standard reference drug, acarbose. © 2026 Deutsche Pharmazeutische Gesellschaft.
Related Docs
View other Related Docs
1. Design, Synthesis, and Α-Glucosidase-Inhibitory Activity of Phenoxy-Biscoumarin–N-Phenylacetamide Hybrids, Archiv der Pharmazie (2021)
2. Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors, Bioorganic and Medicinal Chemistry (2019)
3. Design, Synthesis, Α-Glucosidase Inhibition and Hypoglycemic Activity of 3-Aceto(Benzo)Hydrazide-1,2,4-Triazines As Potential Anti-Diabetic Agents, European Journal of Medicinal Chemistry Reports (2024)
Experts (# of related papers)
View all Related Experts
Mohammad Ali Faramarzi (15)
Mohammad Mahdavi (15)
Other Related Docs
4. Benzimidazole-Phenoxy-1,2,3-Triazole-Benzyl Derivatives As the New Potent Α-Glucosidase Inhibitors: Design, Synthesis, in Vitro, and in Silico Biological Evaluations, Current Organic Synthesis (2025)
5. A New Series of Schiff Base Derivatives Bearing 1,2,3-Triazole: Design, Synthesis, Molecular Docking, and Α-Glucosidase Inhibition, Archiv der Pharmazie (2019)
6. Identification of Novel Triazolopyrimidines As Potent Α-Glucosidase Inhibitor Through Design, Synthesis, Biological Evaluations, and Computational Analysis, Scientific Reports (2025)
7. New Quinoxalin-1,3,4-Oxadiazole Derivatives: Synthesis, Characterization, in Vitro Biological Evaluations, and Molecular Modeling Studies, Archiv der Pharmazie (2021)
8. Design, Synthesis, and Evaluation of the Rhodanine-3-Propanoic Acid-Phenoxy-1,2,3-Triazole-Acetamide Derivatives As Active Agents Against Α-Glucosidase, Α-Amylase, and Protein Tyrosine Phosphatase 1B, Journal of Molecular Structure (2026)
9. Synthesis, Bioactivity, and Molecular Docking of Benzimidazole-2-Carbamate Derivatives As Potent Α-Glucosidase Inhibitors, Journal of Molecular Structure (2023)
10. Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents, Scientific Reports (2024)
11. A Review on Synthesis, Mechanism of Action, and Structure-Activity Relationships of 1,2,3-Triazole-Based Α-Glucosidase Inhibitors As Promising Anti-Diabetic Agents, Journal of Molecular Structure (2022)
12. Quinoline-Piperazine Derivatives As Potential Α-Glucosidase Inhibitors: Synthesis, Biological Evaluation, and in Silico Studies, Journal of Molecular Structure (2025)
13. New Phenylthiosemicarbazide-Phenoxy-1,2,3-Triazole-N-Phenylacetamides As Dual Inhibitors Against Α-Glucosidase and Ptp-1B for the Treatment of Type 2 Diabetes, Archiv der Pharmazie (2024)
14. Discovery of Novel 4,5-Diphenyl-Imidazol-Α-Aminophosphonate Hybrids As Promising Anti-Diabetic Agents: Design, Synthesis, in Vitro, and in Silico Enzymatic Studies, Bioorganic Chemistry (2023)
15. Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives, Archiv der Pharmazie (2020)
16. A New Route to the Synthesis of 2-Hydrazolyl-4-Thiazolidinone Hybrids, Evaluation of Α-Glucosidase Inhibitory Activity and Molecular Modeling Insights, Heliyon (2024)
17. Imidazo[1,2-C]Quinazolines As a Novel and Potent Scaffold of Α-Glucosidase Inhibitors: Design, Synthesis, Biological Evaluations, and in Silico Studies, Scientific Reports (2023)
18. Design and Synthesis of Novel 5-Arylisoxazole-1,3,4-Thiadiazole Hybrids As Α-Glucosidase Inhibitors, Letters in Drug Design and Discovery (2021)
19. Synthesis and Biological Evaluation of New Benzimidazole-1,2,3-Triazole Hybrids As Potential Α-Glucosidase Inhibitors, Bioorganic Chemistry (2020)
20. Synthesis and Biological Assessment of Benzimidazole-Acrylonitrile-1,2,3-Triazole Derivatives As Α-Glucosidase Inhibitors, Bioorganic Chemistry (2025)