几丁质酶抑制剂及噻唑烷酮类化合物合成与农用活性研究进展

几丁质酶 (EC 3.2.1.14) 可催化几丁质降解生成几丁寡糖，在几丁质代谢通路中发挥着重要作用，在昆虫、真菌和线虫等有害生物的生长发育过程中不可或缺。以几丁质酶为潜在靶标，有望开发出具有全新作用机制的新型农药品种。近年来，由于噻唑烷酮类化合物被报道具有包括几丁质酶抑制活性的多种农用生物活性，其合成方法受到广泛关注。本文以亚洲玉米螟几丁质酶 (OfCht) 为代表，对几丁质酶结构特点，典型糖类、肽类、虚拟筛选和天然产物源酶抑制剂，以及几丁质酶与抑制剂的结合方式进行了概要性综述，着重针对噻唑烷-4-酮、2-硫代噻唑烷-4-酮和噻唑-2,4-二酮3种噻唑烷酮类化合物的合成方法和农用生物活性研究进行了归纳总结，进而对噻唑烷酮类化合物在几丁质酶抑制活性方面的应用进行展望，以期为基于昆虫几丁质酶独特结构特点进行合理设计和发现新型噻唑烷酮类几丁质酶抑制剂用于未来农业害虫防治提供参考。

Chitinase inhibitors and synthesis and agricultural bioactivity of thiazolidinones: a review

Chitinase (EC 3.2.1.14) plays an important role in the chitin metabolism process by degrading chitin into chitooligosaccharides. Chitinase is indispensable for the growth and morphogenesis of agricultural pest and disease host such as insect, fungi, nematode, etc. Therefore, Chitinase is one of the most promising target for developing new pesticide with novel molecular mechanism. In recent years, thiazolidinones were reported to possess a variety of agricultural biological activities including chitinase inhibition, so the synthetic methods of thiazolidinones have attracted widely attention. In this review, the chitinases structure represented by those from Ostrinia furnacalis were summarized, as well as the structures of the inhibitors of carbohydrate, peptide, virtual screening, natural-source ones, and their binding mode. The synthetic method and agricultural biological activity of three classes of thiazolidinones were reviewed, including thiazolidin-4-ones, 2-thioxothiazolidin-4-ones, and thiazolidin-2,4-diones. Meanwhile, the application of thiazolidinones is also prospected as chitinase inhibitors. It will provide a guidance for rational design and discovery of novel thiazolidinones as chitinase inhibitors based on insect chitinase structure for agricultural pest control.