喹喔啉衍生物的合成方法及其潜在的抗炎特性。

IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Mini reviews in medicinal chemistry Pub Date : 2024-06-20 DOI:10.2174/0113895575307480240610055622
Anjali -, Payal Kamboj, Mohammad Amir
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引用次数: 0

摘要

喹喔啉分子因其广泛的生物活性而在药物化学领域备受关注,并成为药物发现和开发中的多功能药层。它的结构由苯并吡嗪的双环组成,具有抗菌、抗真菌、抗病毒、抗癌和抗炎等一系列药理特性。本综述总结了合成喹喔啉类化合物的不同策略及其通过不同机制发挥作用的抗炎特性。此外,还讨论了结构活性关系,以确定结构修饰对抗炎潜力的影响。这些分析揭示了最佳活性所需的关键结构特征,从而推动了具有更好抗炎活性的新喹喔啉类似物的设计和合成。喹喔啉类化合物的抗炎特性归因于它们对几种炎症调节因子表达的抑制作用,如环氧化酶、细胞因子、活化 B 细胞的核因子卡帕-轻链-增强因子(NFB)和 p38 丝裂原活化蛋白激酶(p38 MAPK)。此外,还讨论了核因子红细胞 2 相关因子 2(NRF2)的激活剂以及对阿片受体的激动作用。因此,本综述可为今后设计和开发通过不同分子靶点发挥作用的新型喹喔啉衍生物提供模板,使其成为具有更好疗效和安全性的潜在抗炎药物。.
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Synthetic Methods of Quinoxaline Derivatives and their Potential Anti-inflammatory Properties.

Quinoxaline molecule has gathered a great attention in medicinal chemistry due to its vide spectrum of biological activities and emerged as a versatile pharmacophore in drug discovery and development. Its structure comprises bicyclic ring of benzopyrazine and displays a range of pharmacological properties including antibacterial, antifungal, antiviral, anticancer and anti-inflammatory. This review summarizes the different strategies for the synthesis of quinoxalines and their anti-inflammatory properties acting through different mechanisms. Structure activity relationships have also been discussed in order to determine the effect of structural modifications on anti-inflammatory potential. These analyses illuminate critical structural features required for optimal activity, driving the design and synthesis of new quinoxaline analogues with better anti-inflammatory activities. The anti-inflammatory properties of quinoxalines are attributed to their inhibitory action on expression of several inflammatory modulators such as cyclooxygenase, cytokines, nuclear factor kappa-light-chain-enhancer of activated B cells (NFB) and p38 mitogen activated protein kinase (p38 MAPK). Activators of nuclear factor erythroid 2-related factor 2 (NRF2) and agonistic effect on opioid receptors have also been discussed. Hence, this review may provide a future template for the design and development of novel quinoxaline derivatives acting through different molecular targets as potential anti-inflammatory agents with better efficacy and safety profile.

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来源期刊
CiteScore
7.80
自引率
0.00%
发文量
231
审稿时长
6 months
期刊介绍: The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. Mini-Reviews in Medicinal Chemistry covers all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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