Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376356 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
A series of N-hydroxy-N′-phenylthiourea and N-hydroxy-N′-phenylurea analogues were prepared and evaluated as inhibitors of tyrosinase and melanin formation. The most active analogue 1 inhibited mushroom tyrosinase with an IC50 of around 0.29 μM and also retained a substantial potency in cell culture by reducing pigment synthesis by 78%. Therefore, compound 1 could be considered as a promising candidate for preclinical drug development for skin hyperpigmentation application.
Graphical abstractN-Hydroxy-N′-phenylthiourea and N-hydroxy-N′-phenylurea analogues were designed and evaluated as inhibitors of tyrosinase and melanin formation. The structure of the most active analogue 1 is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide