Synthesis of indole-based-thiadiazole derivatives as a potent inhibitor of α-glucosidase enzyme along with in silico study

Jan 28, 2021Bioorganic chemistry

Creating indole-thiadiazole compounds as strong blockers of the alpha-glucosidase enzyme with computer-based analysis

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Abstract

The synthesized indole-based-thiadiazole derivatives exhibited α-glucosidase inhibitory potential with IC values ranging from 0.95 ± 0.05 to 13.60 ± 0.30 µM.

  • Ten derivatives demonstrated the highest inhibitory activity, with IC values of 0.95 ± 0.05 to 4.80 ± 0.20 µM.
  • Acarbose, a standard comparator, showed an IC value of 1.70 ± 0.10 µM.
  • All tested analogs displayed varying degrees of α-glucosidase inhibition.
  • Structure-activity relationships were established based on the substitution patterns on the phenyl ring.
  • Molecular docking studies confirmed binding interactions for the most active compounds.
  • Kinetic studies indicated that analogs 1, 2, 9, and 17 function as non-competitive inhibitors.

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