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Rational Design of New Quinoline-Benzimidazole Scaffold Bearing Piperazine Acetamide Derivatives As Antidiabetic Agents Publisher Pubmed

Summary: Can a molecule control diabetes? A study found a quinoline-benzimidazole compound is 28 times better than standard drugs at managing blood sugar. #DiabetesCare #DrugDiscovery

Ghasemi M1 ; Iraji A2, 3 ; Dehghan M4 ; Lotfi Nosood Y1 ; Irajie C5 ; Bagherian Khouzani N6 ; Mojtabavi S7 ; Faramarzi MA7 ; Mahdavi M8 ; Alharrasi A1
Authors

Source: Bioorganic Chemistry Published:2024


Abstract

In this study, a series of fifteen compounds (7a–o) based on a quinoline-benzimidazole scaffold bearing piperazine acetamide derivatives were synthesized and evaluated for their potential as α-glucosidase inhibitors, which are important therapeutic agents in the management of type 2 diabetes mellitus. Among the synthesized compounds, 7m exhibited the most potent inhibitory activity, demonstrating a 28-fold greater efficacy than the standard clinical inhibitor, acarbose. Molecular docking studies indicated strong binding interactions between 7m and the α-glucosidase active site, including hydrogen bonding, π–π stacking, and π-cation interactions. Furthermore, molecular dynamics simulations revealed that compound 7m formed a highly stable complex with the enzyme. These findings suggest that compound 7m is a promising candidate for further development as an effective antidiabetic agent, offering valuable insights into the design of potent α-glucosidase inhibitors based on the quinoline-benzimidazole framework. © 2024 Elsevier Inc.
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