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  • Title: Synthesis, biological evaluation and molecular docking study of N-arylbenzo[d]oxazol-2-amines as potential α-glucosidase inhibitors.
    Author: Wang G, Peng Z, Wang J, Li J, Li X.
    Journal: Bioorg Med Chem; 2016 Nov 01; 24(21):5374-5379. PubMed ID: 27614916.
    Abstract:
    A novel series of N-arylbenzo[d]oxazol-2-amines (4a-4m) were synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 4f-4i, 4k and 4m displayed potent inhibitory activity against α-glucosidase with IC50 values in the range of 32.49±0.17-120.24±0.51μM as compared to the standard drug acarbose. Among all tested compounds, compound 4g having 4-phenoxy substitution at the phenyl ring was found to be the most active inhibitor of α-glucosidase with an IC50 value of 32.49±0.17μM. Analysis of the kinetics of enzyme inhibition indicated that compound 4g is a noncompetitive inhibitor of α-glucosidase with a Ki value of 31.33μM. Binding interaction of compound 4g with α-glucosidase was explored by molecular docking simulation.
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