香芹酚类似物的生物学功效。

Q3 Medicine
Zintle Mbese, Blessing Atim Aderibigbe
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引用次数: 7

摘要

背景:香芹酚是植物精油的主要成分。它具有抗菌、抗氧化、抗癌、抗炎和抗胆碱酯酶活性。香芹酚的类似物可以通过选定的合成路线制备,从而得到有效的化合物。目的:通过引入特定的功能修饰香芹酚,有可能提高香芹酚的生物活性。香芹酚上的羟基、苯环和烷基等官能团可以被修饰或用于与重要的药物支架的杂交。结果:在所引专利EP1053744B1中,对羟基进行修饰,并在苯环上引入烯丙基,得到了具有抗菌活性的香菜酚类似物。羟基的修饰影响了类似物的疏水性和环取代基的大小。疏水性和环取代基的大小影响类似物与细菌细胞的相互作用。香芹酚类似物的抗癌活性受其苯环取代基位置的影响。在邻位和对位上引入取代基比在中间位置上引入取代基的取代基具有更好的抗肿瘤活性。结论:基于一些关于卡瓦罗罗类似物的报道,对卡瓦罗罗类似物开发的更多研究将会产生有效的化合物来克服目前在细菌感染、癌症、真菌感染等疾病的治疗中所面临的挑战。然而,为了充分了解这些类似物对选定病原体的作用模式,需要更多的生物学评价。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Biological Efficacy of Carvacrol Analogues.

Background: Carvacrol is the major constituent of essential oils derived from plants. It exhibits antimicrobial, antioxidant, anticancer, anti-inflammatory, and anticholinesterase activity. The analogues of carvacrol can be prepared via selected synthetic routes, resulting in potent compounds.

Objective: Modifying carvacrol by the introduction of selected functionalities has the potential to enhance the biological activity of carvacrol. The functionalities on carvacrol such as the hydroxyl group, benzene ring and alkyl groups can be modified or used for hybridization with important pharmaceutical scaffolds.

Results: In one of the patents cited, EP1053744B1, the modification of the hydroxyl group and the introduction of allyl groups into the benzene ring resulted in carvacrol analogues with antibacterial activity. Modifying the hydroxyl group influenced the hydrophobicity of the analogues and the size of the ring substituent. The hydrophobicity and the size of the ring substituent influence the analogues interactions with bacterial cells. The analogues of carvacrol with anticancer activity were influenced by the position of the substituted groups on the benzene ring. Substituent introduced at the ortho and para- positions resulted in better antitumor activity when compared to the ones with substituents on the meta-position.

Conclusion: Based on several reports on cavarcrol analogues, more research on the development of carvacrol analogues will result in potent compounds that can overcome drug resistance which is currently a challenge in the treatment of diseases, such as bacterial infections, cancer, fungal infections etc. However, more biological evaluation is required in order to fully understand the mode of action of these analogues on selected pathogens.

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来源期刊
Recent patents on anti-infective drug discovery
Recent patents on anti-infective drug discovery Medicine-Pharmacology (medical)
CiteScore
2.40
自引率
0.00%
发文量
1
期刊介绍: Recent Patents on Anti-Infective Drug Discovery publishes review articles on recent patents in the field of anti-infective drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-infective drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-infective drug design and discovery.
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