Synthesis of Amino Acid Derivatives of Kojic Acid and Their Tyrosinase Inhibitory Activity..

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Abstract

Six N-carbobenzozy amino acid derivatives of kojic acid were synthesized to improve the tyrosinase inhibitory activity of kojic acid. All derivatives showed stronger activities than kojic acid. Among them, the L-phenylalanine derivative was the strongest inhibitor and its IC50 value was about 1/80 that for kojic acid. Theinhibition mechanism of these derivatives is considered to be a noncompetitive one similar to that of kojic acid.

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