A series of 1-(1-arylethylidene)thiosemicarbazide compounds and their analogues were synthesized and characterized by 1H NMR, MS. Their tyrosinase inhibitory activities were investigated by an assay based on the catalyzing ability of tyrosinase for the oxidation of L-DOPA, comparing with 4-methoxycinnamic acid and arbutin. The results showed that (1) all the synthesized compounds could perform a significant inhibitory activity for tyrosinase; (2) for these compounds, the main active moiety interacting with the center of tyrosinase would be thiosemicarbazo group; (3) the inhibitory activity was close related with thiosemicarbazide moieties and the groups attached on the aromatic ring.