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合成,表征和抗氧化活性评估新的N-甲基替代的醇衍生的多化合物

Alexandra Cătălina Cornea¹, Gabriel Marc², Ioana Ionuț¹

¹Department of Pharmaceutical Chemistry, "Iuliu Hațieganu" University of Medicine and Pharmacy, 41 Victor Babeș Street, RO-400012 Cluj-Napoca, Romania.

Molecules (Basel, Switzerland)

|March 27, 2025

概括

合成了新的 thiazolyl-polyphenolic 化合物,以对抗活性氧物种. 化合物7j和7k表现出优异的抗氧化活性,为抗氧化压力相关疾病提供新的治疗剂的潜力.

科学领域:

药用化学医学化学
有机合成有机合成
药理学药理学是指药理学的学科.

背景情况:

反应性氧物种 (ROS) 涉及到许多病理,需要强大的抗氧化剂.
多提供抗氧化功效,但稳定性和生物可用性不佳.
需要新的合成策略来克服这些治疗应用的限制.

研究的目的:

为了合成和描述新型的 thiazolyl-polyphenolic 化合物.
评估这些化合物的 in silico 和 in vitro 抗氧化能力.
探索结构-活性关系以增强抗氧化特性.

主要方法:

多步合成包括汉茨赫异环化.
通过NMR,MS和IR光谱进行结构性表征.
在的热力学计算 (HOMO-LUMO,BDE).
在体外抗氧化剂测定 (ABTS,DPPH,RP,TAC,FRAP,CUPRAC).

主要成果:

新型 thiazolyl-polyphenolic 化合物 7a-k 已成功合成和表征.
在分析预测了有利的抗氧化剂配置文件,独立于 thiazole 环位置 2 替换.
化合物7j和7k在体外表现出与 Askorbic 酸和Trolox 相比显著增强的抗氧化活性.

结论:

合成的 thiazolyl-polyphenols 具有强大的抗氧化特性.
对 thiazole 支架的战略性修改可以导致改进的治疗剂.
化合物7j和7k代表了在治疗与氧化压力相关的疾病方面进一步发展的有希望的候选者.

关键词:

在 DFT 方面,它是最重要的.汉茨赫的异环化.这就是ROSOS ROS.抗氧化剂是一种抗氧化剂.在体外 (in vitro) 的情况下.氧化应激是一种氧化应激.聚醇是一种多醇.醇的衍生品醇的衍生品

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