Archiv der Pharmazie · 2026
Synthesis of Some Novel Chalcone and 3,5-Disubstituted Pyrazoline Derivatives: Evaluation of Their α-Amylase and α-Glucosidase Inhibitory Activities In Vitro and In Silico.
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Erbay Fatma, Akatin Melike Yildirim, Demir Fatma, Kahriman Nuran, Colak Ahmet, Ertunga Nagihan Saglam, Küçük Murat
Аннотация
This study reports the synthesis of some novel chalcone (C1-C3) and 3,5-disubstituted pyrazoline derivatives (P1-P3), structurally based on aminophenyl and trifluoromethylphenyl groups. Their potential as antidiabetic agents was evaluated through in vitro inhibition of α-amylase and α-glucosidase enzymes and supported by molecular docking studies. Among all the compounds, P2 showed potent dual inhibition, with IC50 values of 9.35 and 2.10 µM against α-amylase and α-glucosidase, respectively, comparable to or better than the standard inhibitor acarbose. Kinetic studies revealed that P2 acts via a non-competitive mechanism for both enzymes. Docking analysis was performed for all of the molecules. These findings suggest that especially P2 has significant potential as a lead compound for further antidiabetic drug development.