Design and synthesis of new fused carbazole-imidazole derivatives as anti-diabetic agents: In vitro alpha-glucosidase inhibition, kinetic, and in silico studies

摘要

Twenty three fused carbazole-imidazoles 6a-w were designed, synthesized, and screened as new alpha-glucosidase inhibitors. All the synthesized fused carbazole-imidazoles 6a-w were found to be more active than acarbose (IC50 = 750.0 +/- 1.5 mu M) against yeast alpha-glucosidase with IC50 values in the range of 74.0 +/- 0.7-298.3 +/- 0.9 mu M. Kinetic study of the most potent compound 6v demonstrated that this compound is a competitive inhibitor for alpha-glucosidase (K-i value = 75 mu M). 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 alpha-glucosidase.