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Introduction of New Quinolone-2-Thio-Acetamide-Propane Hydrazide-Benzimidazole Derivatives As New Α-Glucosidase and Α-Amylase Inhibitors Publisher



P Nikfar PARISA ; S Karimian SOMAYE ; S Safapoor SAJEDEH ; M Noori MILAD ; N Dastyafteh NAVID ; Sn Ghafouri Seyedeh NILOUFAR ; M Mohammadikhanaposhti MARYAM ; Ba Larijani Bagher A ; P Taslimi PARHAM ; M Mahdavic MOHAMMAD
Authors

Source: Scientific Reports Published:2025


Abstract

In the present work, new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives 12a-o were assigned as potent anti-diabetic agents that targeting α-glucosidase and α-amylase as two important targets in treatment of type 2 diabetes. General scaffold of these compounds was designed based on the reported potent α-glucosidase and α-amylase inhibitors and derivation was performed in acetamide moiety. In vitro evaluation of the new compounds 12a-o demonstrated that most of the synthesized compounds were more potent than standard inhibitor acarbose against α-glucosidase while all these new compounds were more potent than acaerbose against α-amylase. The most potent compound against both studied enzymes was compound 12n that was a 4-fluorophenylacetamide derivative. This compound was 5 and 23.8 folds more potent than acarbose against α-glucosidase and α-amylase, respectively, and with excellent binding energies in comparison to acarbose attached to active sites of these enzymes. Molecular dynamics and pharmacokinetic studies of compound 12n was also performed. © 2025 Elsevier B.V., All rights reserved.
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