In vitro evaluation of 2-pyrazoline derivatives as DPP-4 inhibitors

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Temel H. E., Altıntop M. D., Sever B., Özdemir A., Akalın Çiftçi G.

TURKISH JOURNAL OF BIOCHEMISTRY-TURK BIYOKIMYA DERGISI, sa.1, ss.104-109, 2023 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Basım Tarihi: 2023
  • Doi Numarası: 10.1515/tjb-2022-0161
  • Dergi Adı: TURKISH JOURNAL OF BIOCHEMISTRY-TURK BIYOKIMYA DERGISI
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, EMBASE, Food Science & Technology Abstracts, Directory of Open Access Journals
  • Sayfa Sayıları: ss.104-109
  • Anahtar Kelimeler: cytotoxicity, diabetes mellitus, dipeptidyl peptidase-4, molecular docking, pyrazoline, DIABETES-MELLITUS, PYRAZOLINE, COVID-19
  • Anadolu Üniversitesi Adresli: Evet

Özet

Objectives In this study, the synthesis of three pyrazoline derivatives and the evaluation of their inhibitory effects on dipeptidyl peptidase (DPP-4) were aimed. Materials and methods Pyrazoline-based compounds (1-3) were obtained via the reaction of 1-(2-furyl)-3-(1,3-benzodioxol-5-yl)-2-propen-1-one with 4-substituted phenylhydrazine hydrochloride. The DPP-4 inhibitory effects of compounds 1-3 were determined with a fluorometric assay using Gly-Pro-Aminomethylcoumarin as the fluorogenic substrate. The cytotoxicity of compounds 1-3 on L929 mouse fibroblast (healthy) cell line was evaluated using MTT assay. Results 1-(4-Methylsulfonylphenyl)-3-(2-furyl)-5-(1,3-benzodioxol-5-yl)-2-pyrazoline (2) exhibited the highest DPP-4 inhibitory activity (IC50=5.75 +/- 0.35 mu M). Moreover, compound 2 exerted no significant cytotoxicity against L929 cells (IC50=34.33 +/- 7.09 mu M). Conclusions Target compounds exhibited moderate DPP-4 inhibitory activity and compound 2 was identified as the most active compound.