Synthesis & alpha-glucosidase inhibitory & glucose consumption-promoting activities o flavonoid-coumarin hybrids

摘要

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 alpha-glucosidase and a-amylase dual inhibitors. The kinetic analysis of the most potent alpha-glucosidase inhibitor of each series of compounds revealed that they inhibited alpha-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.