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

Erbay F., Akatin M. Y., DEMİR F., KAHRİMAN N., ÇOLAK A., Ertunga N. S., ...More

Archiv der Pharmazie, vol.359, no.3, 2026 (SCI-Expanded, Scopus) identifier identifier

  • Publication Type: Article / Article
  • Volume: 359 Issue: 3
  • Publication Date: 2026
  • Doi Number: 10.1002/ardp.70222
  • Journal Name: Archiv der Pharmazie
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, Chemical Abstracts Core, Chimica, EMBASE
  • Keywords: chalcones, molecular modeling, pyrazolines, α-amylase inhibition, α-glucosidase inhibition
  • Karadeniz Technical University Affiliated: Yes

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 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.