Four series of derivatives of vanillin,anisaldehyde,genistein and aloe emodin were prepared.The single crystal of (E)-1-(5-(4-methoxyphenyl)-3-(4-methoxystyryl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone,which was synthesized from vanillin, was obtained by spontaneous evaporation method.All the compounds were tested for the tyrosinase inhibitory activities.The results demonstrated that the IC_(50)values of vanillin,anisaldehyde,genistein and aloe emodin against mushroom tyrosinase activity are 68,49,343 and 160μM,respectively.Among the twelve derivatives,(E)-1-(5-(4-methoxyphenyl)-3-(4-methoxystyryl)-4,5- dihydro-1H-pyrazol-1-yl)ethanone from vanillin and 4,5-dimethoxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid from aloe emodin showed good inhibition against the tyrosinase with IC_(50)values of 18μM and 21μM,respectively.