New imidazole compounds are tyrosinase inhibitors useful to treat e.g. melasma, chloasma, lentigines, senile lentigo, and vitiligo, and to prevent and/or treat the signs of ageing

摘要

Imidazole compounds (I) are new. Imidazole compounds compounds of formula (I) are new. R1H, 1-6C alkyl, aryl or aralkyl; and R2, R3H, 1-6C alkyl or aryl. Independent claims are included for: (1) the preparation of (I); and (2) a cosmetic/pharmaceutical composition comprising (I) with a carrier. [Image] ACTIVITY : Dermatological; Cytostatic; Nootropic. MECHANISM OF ACTION : Tyrosinase inhibitor. The tyrosinase inhibiting activity of 2-[(1-hydroxy-5-(4'-fluorophenyl)-1H-imidazol-2-yl)-dithio]-5-(4'-fluorophenyl)-1H-imidazol-1-ol was tested in B16F1 murine melanoma cells using biological assay. The results showed that 2-[(1-hydroxy-5-(4'-fluorophenyl)-1H-imidazol-2-yl)-dithio]-5-(4'-fluorophenyl)-1H-imidazol-1-ol exhibited IC50 value of 0.4279.