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