4.5 Article

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

期刊

FUTURE MEDICINAL CHEMISTRY
卷 15, 期 1, 页码 25-42

出版社

Newlands Press Ltd
DOI: 10.4155/fmc-2022-0184

关键词

antidiabetic; indolin-2-one; in silico; in vitro; kinetics; synthesis

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This study aimed to identify substituted indolin-2-one-based inhibitors for alpha-amylase and alpha-glucosidase. Synthetic compounds were confirmed and evaluated for enzyme inhibition activities, yielding good-to-moderate inhibitory potential. Compounds 1, 2, 6, 16 and 17 showed potent alpha-glucosidase inhibitory activity and could serve as potential lead molecules for antidiabetic agents.
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, alpha-amylase and alpha-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 alpha-glucosidase inhibitors (IC50 = 9.15 +/- 0.12-13.74 +/- 0.12 mu M). Conclusion: This study identified that these synthetic compounds might serve as potential lead molecules for antidiabetic agents.

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