苯并恶唑是药物发现中应用最广泛的杂环化合物之一。天然存在和合成的苯并恶唑显示出广泛的生物活性。许多苯并恶唑可用于治疗多种疾病，迄今为止，其中一些正在进行临床试验。此外，越来越多的苯并恶唑衍生物正在药物发现的早期阶段进行研究，并作为潜在的热门化合物或先导化合物。这一观点试图彻底回顾过去 5 年（2019 年至今）在癌症、神经系统疾病和炎症方面开发的最著名的苯并恶唑的合理设计、构效关系和生物活性。我们还简要概述了每个靶点及其在疾病中的作用。大量的研究工作表明该支架的巨大潜力以及科学界对含有苯并恶唑核心的新型生物活性化合物的高度兴趣。© 2024。作者，获得 Springer Nature Switzerland AG 的独家许可。

The benzoxazole is one of the most widely exploited heterocycles in drug discovery. Natural occurring and synthetic benzoxazoles show a broad range of biological activities. Many benzoxazoles are available for treating several diseases, and, to date, a few are in clinical trials. Moreover, an ever-increasing number of benzoxazole derivatives are under investigation in the early drug discovery phase and as potential hit or lead compounds. This perspective is an attempt to thoroughly review the rational design, the structure-activity relationship, and the biological activity of the most notable benzoxazoles developed during the past 5 years (period 2019-to date) in cancers, neurological disorders, and inflammation. We also briefly overviewed each target and its role in the disease. The huge amount of work examined suggests the great potential of the scaffold and the high interest of the scientific community in novel biologically active compounds containing the benzoxazole core.© 2024. The Author(s), under exclusive licence to Springer Nature Switzerland AG.