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Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents Publisher



Mohammadikhanaposhtani M1 ; Noori M2 ; Valizadeh Y2 ; Dastyafteh N2 ; Ghomi MK2 ; Mojtabavi S3 ; Faramarzi MA3 ; Hosseini S4 ; Biglar M2 ; Larijani B2 ; Rastegar H5 ; Hamedifar H6 ; Mirzazadeh R7 ; Mahdavi M2
Authors

Source: ChemistrySelect Published:2022


Abstract

In this work, novel anti-α-glucosidase agents, thieno[2,3-b]quinoline-acetamide derivatives 5 a–m have been designed and synthesized. These compounds were evaluated in vitro against yeast α-glucosidase. Most of the title new compounds exhibited a significant α-glucosidase inhibitory activity in comparison to positive control, acarbose. In this regards, the most potent compound amongst the tested compounds, compound 5 k, with IC50=48.66±0.02 μM was 15.6-fold more potent than acarbose. Compound 5 k was a competitive inhibitor into α-glucosidase and interacted with important residues of the active site of this enzyme. Three most potent compounds among the newly synthesized compounds 5 j–k and 5 m were evaluated in silico in term of the oral druglikeness and pharmacokinetic properties. The obtained results predicted that these compounds had satisfactory oral druglikeness and pharmacokinetic properties. © 2022 Wiley-VCH GmbH.
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