Synthetic piperidine-substituted chalcones as potential hits for α-amylase inhibitory and antioxidant activities

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 a-amylase inhibitory and 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2 '-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical-scavenging activities. Results: Compared with the standard acarbose, all compounds inhibited a-amylase, with IC50 values of 9.86-35.98 mu M. Docking studies revealed an important 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.

Automated summary

In this study, various piperidinyl-substituted chalcones were synthesized and tested for their inhibitory activity against α-amylase, DPPH, and ABTS radicals. All compounds showed significant inhibition of α-amylase compared to the standard drug acarbose, with IC50 values ranging from 9.86 to 35.98 μM. Docking studies revealed a crucial binding interaction with the enzyme's catalytic site. Moreover, the compounds exhibited promising radical-scavenging potential against DPPH and ABTS radicals. These findings suggest that the synthesized compounds have the potential to be further developed as antidiabetic agents.