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Synthetic benzofuran-linked chalcones with dual actions: a potential therapeutic approach to manage diabetes mellitus.

Irfan AliRafaila RafiqueKhalid Mohammed KhandSridevi ChigurupatiXingyue JiAbdul WadoodUzma SalarSuliman A AlmahmoudAshfaq Ur RehmanShatha Ghazi FelembanShehryar HameedShahnaz Perveen
Published in: Future medicinal chemistry (2023)
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 α-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 α-amylase inhibitory activity ranging from IC 50  = 12.81 ± 0.03 to 87.17 ± 0.15 μM, compared with the standard acarbose (IC 50  = 13.98 ± 0.03 μM). Compounds also demonstrated radical scavenging potential against DPPH and ABTS radicals. Conclusion: The identified compounds may serve as potential leads for further advanced research.
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