Study on the synthesis and biological activity assessment of kojic acid sulfide schiff base.

ABSTRACT: In this study, twenty-six novel kojic acid derivatives were designed and synthesized based on the strategy of preserving kojic acid's active site for interaction with tyrosinase and the principle of active fragment assembly. Among all the synthesis compounds, compound 6a exhibited the most powerful inhibitory effect with an IC₅₀ value of 1.43 ± 0.39 µM, over 18-fold more potent than the parent compound kojic acid (IC₅₀ = 26.09 ± 0.05 µM). The findings from the mechanism of action study suggested that the compound 6a functions as a competitive inhibitor, exhibiting a K_i value of 0.84 µM. The copper ion chelation and fluorescence quenching experiments further demonstrated that 6a interacts with the Cu²⁺ active center of tyrosinase, thereby influenc

SUBMITTER: Yang C 

PROVIDER: S-EPMC12615588 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature