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  • Title: Synthesis & α-glucosidase inhibitory & glucose consumption-promoting activities of flavonoid-coumarin hybrids.
    Author: Sun H, Song X, Tao Y, Li M, Yang K, Zheng H, Jin Z, Dodd RH, Pan G, Lu K, Yu P.
    Journal: Future Med Chem; 2018 May 01; 10(9):1055-1066. PubMed ID: 29676183.
    Abstract:
    AIM: The research of novel and potent antidiabetic agents is urgently needed for the control of the exploding diabetic population. We previously reported the synthesis and antidiabetic activity of natural 8-(6"-umbelliferyl)-apigenin (1), but its antidiabetic targets are not known. Therefore, four series of derivatives were synthesized and evaluated for their antidiabetic activities. Results & methodology: Compounds (5a) and (14a) were identified as new α-glucosidase and α-amylase dual inhibitors. The kinetic analysis of the most potent α-glucosidase inhibitor of each series of compounds revealed that they inhibited α-glucosidase in irreversible modes. In addition, compounds (5a) and (14a) showed potent glucose consumption-promoting activity. CONCLUSION: Compounds (5a) and (14a) could be regarded as promising starting points for the development of antidiabetic candidates.
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