N-Benzylbenzamides: A new class of potent tyrosinase inhibitors

A series of potent inhibitors of tyrosinase and their structure–activity relationships are described. N-Benzylbenzamide derivatives (1–21) with hydroxyl(s) were synthesized and tested for their tyrosinase inhibitory activity. With this series, compound 15 provided a potent tyrosinase inhibition: it effectively inhibited the oxidation of l-DOPA catalyzed by mushroom tyrosinase with an IC50 of 2.2 μM.