Journal
FUTURE MEDICINAL CHEMISTRY
Volume 15, Issue 1, Pages 167-187Publisher
Newlands Press Ltd
DOI: 10.4155/fmc-2022-0247
Keywords
benzofuran; chalcone; in silico; in vitro; radical scavenger; synthesis; alpha-amylase
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In this study, benzofuran-linked chalcone derivatives were evaluated for their dual action in reducing postprandial hyperglycemia and oxidative stress, showing potential as a therapeutic approach for diabetes mellitus.
Background: Identification of molecules having dual capabilities to reduce postprandial hyperglycemia and oxidative stress is one of the therapeutic approaches to treat diabetes mellitus. In this connection, a library of benzofuran-linked chalcone derivatives were evaluated for their dual action. Methods: A series of substituted benzofuran-linked chalcones (2-33) were synthesized and tested for alpha-amylase inhibitory as well as 2,2-diphenylpicrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activities. Results: All compounds showed alpha-amylase inhibitory activity ranging from IC50 = 12.81 +/- 0.03 to 87.17 +/- 0.15 mu M, compared with the standard acarbose (IC50 = 13.98 +/- 0.03 mu M). Compounds also demonstrated radical scavenging potential against DPPH and ABTS radicals. Conclusion: The identified compounds may serve as potential leads for further advanced research. [GRAPHICS]
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