Biochemical evaluation of novel thiazolone derivatives as dual α-glucosidase/α-amylase inhibitors, anti-inflammatory agents
Year: 2024
Type: article
Abstract: BACKGROUND: Using an analogue-based drug design approach, a number of novel 2-substituted-1,3-thiazolone derivatives (3-10) have been produced and given permission to proceed for their anti-inflammatory properties. In the present paper, the new thiazole derivatives were designed, synthesized, and tested for their alpha-glucosidase, alpha-amylase, and COX-inhibitory activities. Approving the anti-diabetic activity. RESULTS: All the new derivatives were assessed in vitro compared to control (Acarbose) alpha-glucosidase, and alpha-amylase inhibition influence was showed shown through (3, 5, and 7) that were the most effective compounds as α-glucosidase inhibitors. CONCLUSIONS: score near to that of control (Acarbose). Meanwhile, compound (4) exhibited a lower ferric-reducing anti-oxidant power (FRAP) value when compared to the control experiment (ascorbic acid). A molecular docking study approved the binding affinity and mode of binding of compounds (4 and 5) to the α-glucosidase and α-amylase binding pockets.
Source: Future Medicinal Chemistry
Institutions: Zagazig University, Port Said University, Arish University
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W4405884026