Synthesis of N-kojic-amino acid and N-kojic-amino acid-kojiate and their tyrosinase inhibitory activity

Bioorganic & Medicinal Chemistry Letters
1996.0

Abstract

Ten amino acid derivatives of kojic acid were synthesized to improve the tyrosinase inh~itory activity of kojic acid. Almost all derivatives showed stronger activities than kojic acid, and in general, N-kojic-amino acid-kojiate was found to have a higher inhibitory potency than N-kojicamino acid. Among them, the N-kojic-L-phenylalanyl kojiate was the strongest inh~itor and its IC50 value was 1/380 that for kojic acid. The inhibition mechanism of these derivatives is considered to be noncompetitive which is similar to that of kojic acid. Copyright © 1996 Elsevier Science Ltd

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