Liu Jing-Rui, Jiang En-Yu, Sukhbaatar Otgonpurev, Zhang Wei-Hua, Zhang Ming-Zhi, Yang Guang-Fu, Gu Yu-Cheng
Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing, China.
Department of Chemistry, School of Applied Sciences, Mongolian University of Life Sciences, Ulaanbaatar, Mongolia.
Med Res Rev. 2025 Jan;45(1):97-143. doi: 10.1002/med.22078. Epub 2024 Aug 16.
5-(3'-Indolyl)oxazole moiety is a privileged heterocyclic scaffold, embedded in many biologically interesting natural products and potential therapeutic agents. Compounds containing this scaffold, whether from natural sources or synthesized, have demonstrated a wide array of biological activities. This has piqued the interest of synthetic chemists, leading to a large number of reported synthetic approaches to 5-(3'-indolyl)oxazole scaffold in recent years. In this review, we comprehensively overviewed the different biological activities and chemical synthetic methods for the 5-(3'-indolyl)oxazole scaffold reported in the literatures from 1963 to 2024. The focus of this study is to highlight the significance of 5-(3'-indolyl)oxazole derivatives as the lead compounds for the lead discovery of anticancer, pesticidal, antimicrobial, antiviral, antioxidant and anti-inflammatory agents, to summarize the synthetic methods for the 5-(3'-indolyl)oxazole scaffold. In addition, the reported mechanism of action of 5-(3'-indolyl)oxazoles and advanced molecules studied in animal models are also reviewed. Furthermore, this review offers perspectives on how 5-(3'-indolyl)oxazole scaffold as a privileged structure might be exploited in the future.
5-(3'-吲哚基)恶唑部分是一种具有优势的杂环骨架,存在于许多具有生物学意义的天然产物和潜在治疗剂中。含有这种骨架的化合物,无论是天然来源还是合成的,都已显示出广泛的生物活性。这激发了合成化学家的兴趣,导致近年来有大量关于5-(3'-吲哚基)恶唑骨架的合成方法报道。在本综述中,我们全面概述了1963年至2024年文献中报道的5-(3'-吲哚基)恶唑骨架的不同生物活性和化学合成方法。本研究的重点是强调5-(3'-吲哚基)恶唑衍生物作为抗癌、杀虫、抗菌、抗病毒、抗氧化和抗炎剂先导发现的先导化合物的重要性,总结5-(3'-吲哚基)恶唑骨架的合成方法。此外,还综述了已报道的5-(3'-吲哚基)恶唑的作用机制以及在动物模型中研究的先进分子。此外,本综述还对5-(3'-吲哚基)恶唑骨架作为一种优势结构在未来如何被利用提供了展望。