Sixteen new acylhydrazone derivatives and twelve intermediates were synthesized using substituted aromatic acids as the staring materials. The structures of the target compounds and intermediates were characterized by IR, NMR and elemental analyses. And that the geometrical isomers of target compounds undergo a rapid cis/trans equilibrium, with the trans conformer predominating at room temperature. The auxin activity test showed that the target compounds have different effect on wheat gemma, the antibacterial activity was present in almost all the target compounds, but better activity was observed against Staphylococcus aureus than Escherichia coli. Particularly compound 4h exhibits higher antibacterial activity to Staphylococcus aureus than the others. The minimal inhibitory concentration (MIC) of 4h with Staphylococcus aureus is 3.13 μg/mL which is similar with chloramphenicol.