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Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies Publisher Pubmed



Adib M1 ; Peytam F1 ; Shourgeshty R1 ; Mohammadikhanaposhtani M2 ; Jahani M1 ; Imanparast S3 ; Faramarzi MA3 ; Larijani B4 ; Moghadamnia AA2, 5 ; Esfahani EN6 ; Bandarian F6 ; Mahdavi M4
Authors

Source: Bioorganic and Medicinal Chemistry Letters Published:2019


Abstract

Twenty three fused carbazole–imidazoles 6a–w were designed, synthesized, and screened as new α-glucosidase inhibitors. All the synthesized fused carbazole-imidazoles 6a-w were found to be more active than acarbose (IC 50 = 750.0 ± 1.5 µM) against yeast α-glucosidase with IC 50 values in the range of 74.0 ± 0.7–298.3 ± 0.9 µM. Kinetic study of the most potent compound 6v demonstrated that this compound is a competitive inhibitor for α-glucosidase (K i value = 75 µM). Furthermore, the in silico studies of the most potent compounds 6v and 6o confirmed that these compounds interacted with the key residues in the active site of α-glucosidase. © 2019
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