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

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• 作者：Marc Criton ; Vé ; ronique Le Mellay-Hamon
• 关键词：Melanin ; Tyrosinase inhibitors ; Phenylthiourea ; N-Hydroxy-N′ ; -phenylthiourea and N-hydroxy-N′ ; -phenylurea derivatives
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：15 June 2008
• 年：2008
• 卷：18
• 期：12
• 页码：3607-3610
• 全文大小：175 K

文摘

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.