A new series of (E)-1-(4-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-3-phenylprop-2-en-1-one 1a(4-((1-benzyl-1H-1,2,3-triazol-4-yl) methoxy)phenyl)-1-phenylprop-2-en-1-one 1b-15b were designed, synthesized based on click chemistry, and biologically evaluated for their activity on tyrosinase. The result showed that most of prepared compounds 1a-15a have potent activating effect on tyrosinase, especially for 3a, 8a-10a and 14a-15a. Among them, compounds 10a and 14a demonstrated the best activity with EC50=1.71 and 5.60 mu molL(-1) respectively, even better than the positive control 8-MOP (EC50=14.8 mu molL(-1)). Conversely, compounds 3b, 5b-6b, 9b-10b, and 15b induced enzymatic inhibition on tyrosinase.