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

Future Med Chem. 2023 Jan;15(1):25-42. doi: 10.4155/fmc-2022-0184. Epub 2023 Jan 16.

Abstract

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 (IC50 = 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.

Keywords: antidiabetic; in silico; in vitro; indolin-2-one; kinetics; synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Glycoside Hydrolase Inhibitors* / chemistry
  • Humans
  • Hypoglycemic Agents* / chemistry
  • Indoles / pharmacology
  • Molecular Docking Simulation
  • Structure-Activity Relationship

Substances

  • Hypoglycemic Agents
  • indolin-2-one
  • Glycoside Hydrolase Inhibitors
  • Indoles