Bioorganic & medicinal chemistry letters

Analogues of N-hydroxy-N′-phenylthiourea and N-hydroxy-N′-phenylurea as inhibitors of tyrosinase and melanin formation

M Criton, V Le Mellay-Hamon

文献索引：Criton, Marc; Le Mellay-Hamon, Veronique Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 12 p. 3607 - 3610

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被引用次数: 51

摘要

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 ...