New halogenated phenylcoumarins as tyrosinase inhibitors

With the aim to find out structural features for the tyrosinase inhibitory activity, in the present communication we report the synthesis and pharmacological evaluation of a new series of phenylcoumarin derivatives with different number of hydroxyl or ether groups and bromo substituent in the scaffold. The synthesized compounds 5–12 were evaluated as mushroom tyrosinase inhibitors showing, two of them, lower IC50 than the umbelliferone. Compound 12 (IC50 = 215 μM) is the best tyrosinase inhibitor of this series.

Graphical abstractWith the aim to find out structural features for the tyrosinase inhibitory activity, in the present communication we report the synthesis and pharmacological evaluation of a new series of phenylcoumarin derivatives with different number of hydroxyl or ether groups and bromo substituent in the scaffold. The synthesized compounds 5–12 were evaluated as mushroom tyrosinase inhibitors showing, two of them, lower IC50 than the umbelliferone. Compound 12 (IC50 = 215 μM) is the best tyrosinase inhibitor of this series.Figure optionsDownload full-size imageDownload as PowerPoint slide