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香豆素的合成、反应活性及生物学应用

Syntheses, reactivity, and biological applications of coumarins.

作者信息

Citarella Andrea, Vittorio Serena, Dank Christian, Ielo Laura

机构信息

Dipartimento di Chimica, Università degli Studi di Milano, Milano, Italy.

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Milano, Italy.

出版信息

Front Chem. 2024 Feb 19;12:1362992. doi: 10.3389/fchem.2024.1362992. eCollection 2024.

Abstract

This comprehensive review, covering 2021-2023, explores the multifaceted chemical and pharmacological potential of coumarins, emphasizing their significance as versatile natural derivatives in medicinal chemistry. The synthesis and functionalization of coumarins have advanced with innovative strategies. This enabled the incorporation of diverse functional fragments or the construction of supplementary cyclic architectures, thereby the biological and physico-chemical properties of the compounds obtained were enhanced. The unique chemical structure of coumarine facilitates binding to various targets through hydrophobic interactions pi-stacking, hydrogen bonding, and dipole-dipole interactions. Therefore, this important scaffold exhibits promising applications in uncountable fields of medicinal chemistry (e.g., neurodegenerative diseases, cancer, inflammation).

摘要

本综述涵盖2021年至2023年,探讨了香豆素多方面的化学和药理潜力,强调了它们作为药物化学中多功能天然衍生物的重要性。香豆素的合成和功能化已通过创新策略取得进展。这使得能够引入各种功能片段或构建补充性环状结构,从而增强了所得化合物的生物学和物理化学性质。香豆素独特的化学结构有利于通过疏水相互作用、π-堆积、氢键和偶极-偶极相互作用与各种靶点结合。因此,这个重要的骨架在药物化学的无数领域(如神经退行性疾病、癌症、炎症)展现出了广阔的应用前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2877/10909861/a23ffd29139e/FCHEM_fchem-2024-1362992_wc_sch1.jpg

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