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Design, Synthesis and Bio-Evaluation of Indolin-2-ones As Potential Antidiabetic Agents

Future medicinal chemistry(2023)

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摘要
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.
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关键词
antidiabetic,indolin-2-one,in silico,in vitro,kinetics,synthesis
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