三唑类酪氨酸酶抑制剂的研究进展。

IF 6 2区 医学 Q1 CHEMISTRY, MEDICINAL
Arif Mermer , Serpil Demirci
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引用次数: 3

摘要

酪氨酸酶广泛存在于微生物、动物和植物中,在黑色素生成中具有重要地位,在水果和蔬菜的不良褐变、抗生素耐药性、皮肤色素形成、角质层硬化、神经退行性变等方面发挥着重要作用。因此,酪氨酸酶在食品、农业、,在化妆品和制药工业中,酪氨酸酶已成为开发抗肿瘤、抗癌、抗菌、皮肤美白、杀虫剂等治疗剂的靶酶,近年来大量合成酪氨酸酶抑制剂被广泛报道。三唑环具有广泛的生物作用,在合成新的酪氨酸酶抑制剂方面越来越受到关注。本文综述了1,2,3-或1,2,4-三唑衍生物对酪氨酸酶的抑制作用、构效关系、酶抑制动力学和作用机制。所收集的数据有望为开发新的、有效的和安全的酪氨酸酶抑制剂提供合理的指导和有影响力的策略,以便在未来更好地实际应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Recent advances in triazoles as tyrosinase inhibitors

Recent advances in triazoles as tyrosinase inhibitors

The tyrosinase enzyme, which is widely found in microorganisms, animals and plants, has a significant position in melanogenesis, plays an important role in undesirable browning of fruits and vegetables, antibiotic resistance, skin pigment formation, sclerotization of cuticle, neurodegeneration, etc. Therefore, with the wide potential application fields of tyrosinase in food, agriculture, cosmetics and pharmaceutical industries, which has become the target enzyme for the development of therapeutic agents such as antibrowning, anticancer, antibacterial, skin whitening, insecticides, etc., a large number of synthetic tyrosinase inhibitors have been widely reported in recent years. The triazole ring, which has a broad spectrum of biological action, is of increasing interest in the synthesis of new tyrosinase inhibitors. In this review, tyrosinase inhibition effects, structure-activity relationships, enzyme inhibition kinetics and mechanisms of action of 1,2,3- or 1,2,4-triazole derivatives were investigated. The data gathered is anticipated to supply rational guidance and an influential strategy for the development of novel, potent and safe tyrosinase inhibitors for better practical application in the future.

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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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