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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Authors: Fatma Kübra Erbay, Melike Yıldırım Akatın, F. Merve Demir, Nuran Kahriman, Ahmet Çolak, Nagihan Sağlam Ertunga, Murat Küçük
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References: 42

Abstract

ABSTRACT 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 IC 50 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.

Fields of Study & Subjects

Heterocyclic Compound Synthesis and Bioactivity Natural Antidiabetic Agents Studies Synthesis of Organic Compounds

Publication details

Journal / source
Archiv der Pharmazie
Volume
359
Issue
3
Pages
e70222–e70222
Publication date
1 March 2026
Language
EN