吡啶甲基亚氨基噻(噁)唑烷的合成及生物活性

Synthesis and Bioactivities of Novel Substituted Pyridinylmethylimino-thiazolidines and Oxazolidines Derivatives

摘要: 根据天然海藻糖酶抑制剂的结构设计了一类吡啶甲基亚氨基噻(噁)唑烷化合物, 通过吡啶甲基异硫氰酸酯和相应的胺反应, 然后在盐酸或黄色氧化汞条件下关环,合成了吡啶甲基亚氨基噻唑烷和噁唑烷,其结构得到IR、1H NMR、HRMS的确证。测试了化合物对昆虫(家蝇)飞行的抑制能力。对影响合成反应的因素以及生测结果进行了讨论。

Abstract: Based on the structure of Trehazolin, one of natural trehalase inhibitors, pyridinylmethylimino-thiazolidine and oxazolidine compounds were designed and synthesized through reaction of pyridinylmethyl isothiocyanate with appropriate amine and followed by cyclization under HCl and HgO. Their structures were confirmed by using IR, 1H NMR, HRMS. The insect-flight inhibitory bioactivity was given.