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

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Abstract Objectives In this study, the synthesis of three pyrazoline derivatives and the evaluation of their inhibitory effects on dipeptidyl peptidase (DPP-4) were aimed. 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 (IC 50 =5.75 ± 0.35 µM). Moreover, compound 2 exerted no significant cytotoxicity against L929 cells (IC 50 =34.33 ± 7.09 µM). Conclusions Target compounds exhibited moderate DPP-4 inhibitory activity and compound 2 was identified as the most active compound.