Five-membered heterocycles containing nitrogen, oxygen atoms, especially isoxazoles, are widely present in many natural products and drugs and have relevant medical and pharmaceutical applications. Due to their rich biological activity, the development of novel isoxazole derivatives has been the focus of researchers and scientists. It is worth noting that a large number of isoxazoles have been used frequently as clinical drugs to treat various diseases, showing great development value and wide medicinal potential. In this review, the research progress of isoxazole natural products in anti-bacterial, anti-tuberculosis, anti-virus, anti-tumor, anti-inflammation, anti-diabetes, anti-parasite, anti-psychosis and other biological activities was reviewed. Finally, the research and development prospects of isoxazole natural products were prospected. This review will provide reference for the design of natural isoxazole products with stronger activity and less toxicity.

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天然产物-异恶唑杂化物：药物化学发展回顾

含有氮、氧原子的五元杂环，特别是异恶唑，广泛存在于许多天然产物和药物中，并具有相关的医学和制药应用。由于其丰富的生物活性，新型异恶唑衍生物的开发一直是研究人员和科学家关注的焦点。值得注意的是，大量异恶唑类药物已频繁作为临床药物用于治疗多种疾病，显示出巨大的开发价值和广泛的药用潜力。本文综述了异恶唑天然产物在抗菌、抗结核、抗病毒、抗肿瘤、抗炎、抗糖尿病、抗寄生虫、抗精神病等生物活性方面的研究进展。最后对异恶唑天然产物的研究开发前景进行了展望。该综述将为活性更强、毒性更小的天然异恶唑产品的设计提供参考。