Bioorganic & Medicinal Chemistry Letters 2006-05-15

N-Benzylbenzamides: a new class of potent tyrosinase inhibitors.

Sung Jin Cho, Jung Seop Roh, Won Suck Sun, Sung Han Kim, Ki Duk Park

Index: Bioorg. Med. Chem. Lett. 16 , 2682-4, (2006)

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Abstract

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 IC(50) of 2.2microM.