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Abstract
Background: In medicinal chemistry, searching for new therapeutic entities to treat diabetes mellitus is of great concern. The piperidinyl-substituted chalcone scaffold has piqued our interest as a potential antidiabetic agent. Methods: A variety of piperidinyl-substituted chalcones 2-28 were synthesized and tested for α-amylase inhibitory and2,2-diphenyl-1-picrylhydrazyl (DPPH) and2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical-scavenging activities. Results: Compared with the standard acarbose, all compounds inhibited α-amylase, with IC50 values of 9.86-35.98μM. Docking studies revealed animportant binding interaction with the enzyme's catalytic site. The compounds also demonstrated promising radical-scavenging potential against DPPH and ABTS radicals. Conclusion: This study has identified potential lead candidates for further advanced research searching for antidiabetic agents.
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