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萘酰亚胺作为新药发现的特定支架概述。

An Overview of Naphthylimide as Specific Scaffold for New Drug Discovery.

机构信息

School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, China.

出版信息

Molecules. 2024 Sep 24;29(19):4529. doi: 10.3390/molecules29194529.

Abstract

Naphthylimides play a pivotal role as aromatic heterocyclic compounds, serving as the foundational structures for numerous pharmacologically significant drugs. These drugs encompass antibacterial, antifungal, anticancer, antimalarial, antiviral, anti-inflammatory, antithrombotic, and antiprotozoal agents. The planar and heteroaromatic characteristics of naphthylimides grant them a strong ability to intercalate into DNA. This intercalation property renders naphthylimide derivatives highly valuable for various biological activities. The advantageous pharmacological activity and ease of synthesis associated with naphthylimides and their derivatives provide significant benefits in the design and development of new compounds within this class. Currently, only a few such molecules are undergoing preclinical and clinical evaluations. In this paper, we have compiled the literature on naphthylimides reported by researchers from 2006 to 2024. Our focus lies on exploring the pharmacological activities of their analogues from a drug development and discovery perspective, while examining their structure-activity relationship and mechanisms of action.

摘要

萘酰亚胺作为芳香杂环化合物起着至关重要的作用,是许多具有重要药理作用的药物的基础结构。这些药物包括抗菌、抗真菌、抗癌、抗疟、抗病毒、抗炎、抗血栓和抗原生动物药物。萘酰亚胺的平面和杂芳环特性赋予它们很强的与 DNA 插入的能力。这种插入特性使萘酰亚胺衍生物具有多种生物活性。萘酰亚胺及其衍生物具有有利的药理学活性和易于合成的特点,为该类化合物的新化合物的设计和开发提供了重要的优势。目前,只有少数此类分子正在进行临床前和临床评估。在本文中,我们汇集了 2006 年至 2024 年研究人员报道的萘酰亚胺文献。我们的重点是从药物开发和发现的角度探索其类似物的药理活性,同时研究它们的构效关系和作用机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/69c5/11478049/0858f4910139/molecules-29-04529-g001.jpg

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