Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives

A series of novel 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives were designed, synthesized, and their acrosin inhibitory activities in vitro were evaluated. The results of the acrosin inhibitory activity showed that all target compounds were more potent than the control TLCK. Of all compounds, compound AQ-E5 displayed the most potent acrosin inhibitory activity, with an IC50 of 0.01 μmol/mL and the docking result of compound AQ-E5 within the active site of acrosin was as follows.