The Benzoxazole Heterocycle: A Comprehensive Review of the Most Recent Medicinal Chemistry Developments of Antiproliferative, Brain-Penetrant, and Anti-inflammatory Agents

IF 8.6 2区 化学 Q1 Chemistry Topics in Current Chemistry Pub Date : 2024-10-21 DOI:10.1007/s41061-024-00477-6
Simona Di Martino, Maria De Rosa
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Abstract

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.

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苯并恶唑杂环:抗增殖、脑穿透和抗炎药物的最新药物化学发展综述
苯并恶唑是药物研发中应用最广泛的杂环之一。天然存在和合成的苯并恶唑具有广泛的生物活性。许多苯并噁唑类药物可用于治疗多种疾病,迄今为止,少数药物已进入临床试验阶段。此外,越来越多的苯并恶唑衍生物作为潜在的主打或先导化合物,正在药物发现的早期阶段接受研究。本视角试图全面回顾过去 5 年(2019 年至今)在癌症、神经系统疾病和炎症领域开发的最著名的苯并恶唑的合理设计、结构-活性关系和生物活性。我们还简要概述了每个靶点及其在疾病中的作用。所研究的大量工作表明了该支架的巨大潜力,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浓厚兴趣。
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来源期刊
Topics in Current Chemistry
Topics in Current Chemistry 化学-化学综合
CiteScore
11.70
自引率
1.20%
发文量
0
审稿时长
6-12 weeks
期刊介绍: Topics in Current Chemistry provides in-depth analyses and forward-thinking perspectives on the latest advancements in chemical research. This renowned journal encompasses various domains within chemical science and their intersections with biology, medicine, physics, and materials science. Each collection within the journal aims to offer a comprehensive understanding, accessible to both academic and industrial readers, of emerging research in an area that captivates a broader scientific community. In essence, Topics in Current Chemistry illuminates cutting-edge chemical research, fosters interdisciplinary collaboration, and facilitates knowledge-sharing among diverse scientific audiences.
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