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., ...Daha Fazla

Archiv der Pharmazie, cilt.359, sa.3, 2026 (SCI-Expanded, Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 359 Sayı: 3
  • Basım Tarihi: 2026
  • Doi Numarası: 10.1002/ardp.70222
  • Dergi Adı: Archiv der Pharmazie
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, Chemical Abstracts Core, Chimica, EMBASE
  • Anahtar Kelimeler: chalcones, molecular modeling, pyrazolines, α-amylase inhibition, α-glucosidase inhibition
  • Karadeniz Teknik Üniversitesi Adresli: Evet

Özet

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.