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Dipeptidyl peptidase-4 (DPP-4) inhibition has been recognized as a promising approach to develop safe and potent antidiabetic agents for the management of type 2 diabetes. In this context, new thiosemicarbazones ( 2a - o ) were prepared efficiently by the reaction of aromatic aldehydes with 4-[4-(1 H -pyrazol-1-yl)phenyl]thiosemicarbazide ( 1 ), which was obtained via the reaction of 4-(1 H -pyrazol-1-yl)phenyl isothiocyanate with hydrazine hydrate. Compounds 2a - o were evaluated for their DPP-4 inhibitory effects based on a convenient fluorescence-based assay. 4-[4-(1 H -pyrazol-1-yl)phenyl]-1-(4-bromobenzylidene)thiosemicarbazide ( 2f ) was identified as the most effective DPP-4 inhibitor in this series with an IC 50 value of 1.266 ± 0.264 nM when compared with sitagliptin (IC 50 = 4.380 ± 0.319 nM). MTT test was carried out to assess the cytotoxic effects of compounds 2a - o on NIH/3T3 mouse embryonic fibroblast (normal) cell line. According to cytotoxicity assay, compound 2f showed cytotoxicity towards NIH/3T3 cell line with an IC 50 value higher than 500 µM pointing out its favourable safety profile. Molecular docking studies indicated that compound 2f presented π-π interactions with Arg358 and Tyr666 via pyrazole scaffold and 4-bromophenyl substituent, respectively. Overall, in vitro and in silico studies put emphasis on that compound 2f attracts a great notice as a drug-like DPP-4 inhibitor for further antidiabetic research.

Pyrazole Incorporated New Thiosemicarbazones: Design, Synthesis and Investigation of DPP-4 Inhibitory Effects