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Quinoline-Thiosemicarbazone-1,2,3-Triazole-Acetamide Derivatives As New Potent Α-Glucosidase Inhibitors Publisher Pubmed

Summary: Can new compounds control diabetes? A study found quinoline-triazole derivatives strongly inhibit α-glucosidase, offering potential for better diabetes treatments. #DiabetesResearch #DrugDiscovery

Khademian A1 ; Halimi M2 ; Azarbad R1 ; Alaedini AH3 ; Noori M4 ; Dastyafteh N4 ; Mojtabavi S5 ; Faramarzi MA5 ; Mohammadikhanaposhtani M6 ; Mahdavi M4
Authors

Source: Scientific Reports Published:2024


Abstract

In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC50 = 48.4 µM was 15.5-times more potent than acarbose. According to kinetic study, compound 10n was a competitive inhibitor against α-glucosidase. This compound formed the desired interactions with important residues of the binding pocket of α-glucosidase with favorable binding energy in the molecular docking and molecular dynamics. Compounds 10n, 10e, and 10 g as the most potent compounds among the synthesized compounds were evaluated in term of pharmacokinetics and toxicity via online servers. These evaluations predicted that compounds 10n, 10e, and 10 g had good pharmacokinetic properties and toxicity profile. © The Author(s) 2024.
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