New triazole derivatives, useful e.g. to treat melasma, chloasma, lentigines, senile lentigo, vitiligo, freckles and aging signs and for bodily and hair hygiene, are tyrosinase inhibitors

摘要

Trizole derivatives (I) are new. Triazole derivatives of formula (I) and their salts and tautomeric and geometrical forms are new. R1 = substituted amine, T, T1, T2, T3 or T4; T = 2-10C alkyl, excluding tert-butyl; T1 = 2-10C alkenyl; T2 = aryl radical (optionally substituted), excluding unsubstituted phenyl, 3-bromophenyl, 4-trifluoromethylphenyl, naphthyl, 4-tert-butylphenyl, 3,5-trifluoromethylphenyl, 4-pentylphenyl, 4-chlorophenyl, 3,5-dichlorophenyl, furan-2-yl, thiophen-2-yl, pyridin-3-yl, pyridin-4-yl, pyrazin-2-yl, 4-methoxyphenyl, 4-hydroxyphenyl and 3-hydroxyphenyl; T3 = aralkyl (optionally substituted), excluding benzyl; and T4 = cycloalkyl excluding adamantyl. Independent claims are also included for: (a) method of preparation of (I); and (b) compositions comprising (I). [Image] - ACTIVITY : Dermatological; Nootropic; Antiinflammatory. - MECHANISM OF ACTION : Tyrosinase inhibitor. The ability of (I) to inhibit tyrosinase was tested in B16F1 cells. The results showed that 5-(2-methylpropenyl)-4H-[1,2,4] triazole-3-thiol exhibited an IC50 value of 3.5 mu M.