Discovery of novel 6-(piperidin-1-ylsulfonyl)-2H-chromenes targeting α-glucosidase, α-amylase, and PPAR-γ: Design, synthesis, virtual screening, and anti-diabetic activity for type 2 diabetes mellitus

The synthesized 2H-chromene derivatives demonstrated inhibitory potency against α-glucosidase with values ranging from 90.6% to 96.3% at 100 µg/mL.

• Two derivatives, 6 and 10, showed the highest α-glucosidase inhibitory potency with IC values of 0.975 ± 0.04 and 0.584 ± 0.02 µg/mL, respectively.
• The results indicate that these compounds may be potential α-glucosidase inhibitors, which is relevant for diabetes management.
• The derivatives also exhibited moderate activity on α-amylase and acted as PPAR-γ agonists, suggesting multiple mechanisms for antidiabetic effects.
• The most active compounds, 6 and 10, had IC values of 3.453 ± 0.14 and 4.653 ± 0.04 µg/mL against PPAR-γ, enhancing insulin sensitivity.
• In-silico analysis showed that the compounds complied with Lipinski's and Veber's rules, indicating potential for good oral bioavailability.

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