Literature

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 (IC50 = 750.0 ± 1.5 µM) against yeast α-glucosidase with IC50 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 (Ki 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.

DOI： 10.1016/j.bmcl.2019.01.012

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Bioorganic & Medicinal Chemistry Letters 2019.0

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