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Future Med Chem ; 15(1): 25-42, 2023 01.
Article in English | MEDLINE | ID: mdl-36644975

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.


Subject(s)
Glycoside Hydrolase Inhibitors , Hypoglycemic Agents , Humans , Hypoglycemic Agents/chemistry , Molecular Docking Simulation , Glycoside Hydrolase Inhibitors/chemistry , Indoles/pharmacology , Structure-Activity Relationship
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