Isatin-hydrazide conjugates as potent α-amylase and α-glucosidase inhibitors: Synthesis, structure and in vitro evaluations

Oct 2, 2021Bioorganic chemistry

Isatin-hydrazide compounds as strong blockers of enzymes that break down starch and sugars: Creation, structure, and lab testing

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Abstract

Conjugates 1a, 1h, and 1f exhibit potent α-amylase inhibition with IC values of 19.6, 12.1, and 18.3 µg/ml, respectively.

  • The compounds are novel inhibitors of α-amylase and α-glucosidase derived from isatin.
  • Conjugate 1a demonstrates significant activity against α-glucosidase with an IC value of 14.8 µg/ml.
  • Compounds 1a and 1f show two-fold better inhibitory activity against both enzymes compared to the standard inhibitor, acarbose.
  • Molecular docking studies suggest potential binding modes of the compounds with enzyme active sites.
  • These findings highlight the possibility of these compounds as promising candidates for further research.

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