1-脱氧野尻霉素是一种多羟基生物碱，可竞争性地与α-葡萄糖苷酶结合，除降血糖的研究外，在抗肿瘤、抗病毒、抗氧化方面的研究也逐渐增加。研究者采用多种方法对1-脱氧野尻霉素进行结构修饰，不只在环内N原子上进行结构改造，在骨架其他部位的修饰也逐渐增多，取代基的种类多种多样，烷基链的某些碳原子可以被杂原子或官能团取代，也可以在末端连接其他基团。取代基的不同对活性有一定的影响，同一取代基也可能有不止一种活性，碳原子用杂原子取代对活性提高有帮助，化合物的旋光性也是影响活性的因素。综述了不同种类官能团取代的1-脱氧野尻霉素衍生物及其活性的研究进展，为1-脱氧野尻霉素的结构修饰研究提供参考。

1-Deoxynojirimycin is a polyhydroxy alkaloid that can competitively bind to the α-glucosidase. In addition to hypoglycemic activity, research of 1-deoxynojirimycin on anti-tumor, antiviral, and antioxidant activities is also gradually increasing. Researchers have used various methods to modify the structure of 1-deoxynojirimycin. People not only carry out structural modifications on the N atoms in the ring, but also gradually increase the modification of other parts of the skeleton. There are various types of substituents. Some carbon atoms in the alkyl chain can be substituted by heteroatoms or functional groups, and other groups can also be connected at the end. Different substituents have a certain impact on the activity. The same substituent may also have more than one activity. Substitution of carbon atoms with heteroatoms can help improve the activity. The optical activity of compounds is also a factor that affects the activity. This article reviews the research progress of 1-deoxynojirimycin derivatives with different functional groups and their activities, providing a reference for the structural modification of 1-deoxynojirimycin.

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国家重点研发计划项目（2019YFC1710504）；国家自然科学基金资助项目（82173710）；北京市自然科学基金资助项目（7192129）；中国医学科学院医学与健康科技创新工程项目（2021-I2M-1-028，2022-I2M-2-002）