Novel carbazole-oxadiazole derivatives as anti-α-glucosidase and anti-α-amylase agents: Design, synthesis, molecular docking, and biological evaluation

Jun 18, 2024European journal of medicinal chemistry

New carbazole-oxadiazole compounds as inhibitors of enzymes involved in sugar digestion: design, testing, and computer modeling

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Abstract

Most of the tested carbazole-oxadiazole derivatives displayed varying degrees of α-glucosidase and α-amylase inhibitory activity, with IC values ranging from 21.39 ± 0.69 to 126.14 ± 6.33 μM.

  • Compound 6c exhibited the highest anti-α-glucosidase activity with an IC value of 21.39 ± 0.69 μM.
  • Compound 6e showed the most effective anti-α-amylase activity with an IC value of 45.53 ± 1.50 μM.
  • Lineweaver-Burk plot analysis indicated that 6c acts as a mixed inhibitor of α-glucosidase.
  • 6e was identified as a mixed inhibitor of α-amylase.
  • Molecular docking simulations suggested specific interaction mechanisms for both 6c and 6e with their target enzymes.
  • The potential for reducing postprandial blood glucose levels, along with favorable oral activity and low cytotoxicity, supports the consideration of these compounds as lead candidates for new hypoglycemic agents.

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