Design, synthesis, molecular modeling, and biological evaluation of novel kojic acid derivatives containing bioactive heterocycle moiety as inhibitors of tyrosinase and antibrowning agents

Tyrosinase plays an important role in melanin biosynthesis and enzymatic browning of fresh-cut fruit and vegetables. To discover potent tyrosinase inhibitors and antibrowning agents, a series of novel kojic acid derivatives containing bioactive heterocycle moiety (4a-4l) were designed and synthesized. Thereinto, 4d displayed the most potent tyrosinase inhibitory activity with IC50 of 3.23 ± 0.26 μM and behaved as a competitive inhibitor with a...