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Design, synthesis and bio-evaluation of indolin-2-ones as potential antidiabetic agents.

Itohowo Gabriel AsuquoMehwish SolangiKhalid Mohammed KhandSridevi ChigurupatiIfeanyi Edozie OtuokereFrancis Kalu EkumaUzma SalarShatha Ghazi FelembanAshfaq Ur RehmanAbdul WadoodMuhammad Taha
Published in: Future medicinal chemistry (2023)
Background: Diabetes mellitus is a serious global health concern, and this is expected to impact more than 300 million people by 2025. The current study focuses on identifying substituted indolin-2-one-based inhibitors for two indispensable drug targets, α-amylase and α-glucosidase. Methods: The structures of synthetic compounds were confirmed by spectroscopic techniques and evaluated for enzyme inhibition activities. Kinetic and in silico studies were also performed. Results: All compounds exhibited good-to-moderate inhibitory potential. Most importantly, compounds 1 , 2 , 6 , 16 and 17 were identified as potent α-glucosidase inhibitors (IC 50  = 9.15 ± 0.12-13.74 ± 0.12 μM). Conclusion: This study identified that these synthetic compounds might serve as potential lead molecules for antidiabetic agents.
Keyphrases
  • molecular docking
  • global health
  • public health
  • human health
  • type diabetes
  • high intensity
  • risk assessment
  • weight loss
  • case control