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Hydroxy- or methoxy-substituted benzaldoximes and benzaldehyde-O-alkyloximes as tyrosinase inhibitors.
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2001 Jul Ley, J P, Bertram, H J
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2001 Jul Ley, J P, Bertram, H J
Several benzaldoximes, benzaldehyde-O-ethyloximes, and acetophenonoximes were synthesized and evaluated as tyrosinase inhibitors by an assay based on tyrosinase catalyzed L-DOPA oxidation. Whereas benzaldoxime itself is only a weak inhibitor, its derivatives with one or two hydroxy or methoxy moieties in para and meta positions depress tyrosinase activity. Acetophenonoximes and trisubstituted benzaldoximes show no inhibitory activity. The IC(50) of 3,4-dihydroxybenzaldehyde-O-ethyloxime (0.3 +/- 0.1 micromol L(-1)) is of the same magnitude as tropolone (0.13 +/- 0.08 micromol L(-1)), one of the best tyrosinase inhibitors known so far.
中文翻译:
羟基或甲氧基取代的苯甲醛肟和苯甲醛-O-烷基肟作为酪氨酸酶抑制剂。
合成了几种苯甲醛肟,苯甲醛-O-乙基肟和对乙酰氨基苯甲酸,并通过基于酪氨酸酶催化的L-DOPA氧化的分析,评估它们作为酪氨酸酶抑制剂。苯并肟肟本身仅是一种弱抑制剂,而其对位和间位具有一个或两个羟基或甲氧基部分的衍生物会降低酪氨酸酶的活性。苯乙酮肟和三取代的苯甲醛肟没有抑制活性。3,4-二羟基苯甲醛-O-乙基肟(0.3 +/- 0.1 micromol L(-1))的IC(50)与托酚酮(0.13 +/- 0.08 micromol L(-1))的幅度相同,其中一个迄今为止已知的最佳酪氨酸酶抑制剂之一。
更新日期:2017-01-31
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
羟基或甲氧基取代的苯甲醛肟和苯甲醛-O-烷基肟作为酪氨酸酶抑制剂。
合成了几种苯甲醛肟,苯甲醛-O-乙基肟和对乙酰氨基苯甲酸,并通过基于酪氨酸酶催化的L-DOPA氧化的分析,评估它们作为酪氨酸酶抑制剂。苯并肟肟本身仅是一种弱抑制剂,而其对位和间位具有一个或两个羟基或甲氧基部分的衍生物会降低酪氨酸酶的活性。苯乙酮肟和三取代的苯甲醛肟没有抑制活性。3,4-二羟基苯甲醛-O-乙基肟(0.3 +/- 0.1 micromol L(-1))的IC(50)与托酚酮(0.13 +/- 0.08 micromol L(-1))的幅度相同,其中一个迄今为止已知的最佳酪氨酸酶抑制剂之一。