摘要/Abstract
将N，N-二甲基甲酰胺基引入1，5-苯并硫氮杂(艹卓)，设计合成了6个2-取代苯基-3-（N，N-二甲基甲酰胺基）-4-甲基-1，5-苯并硫氮杂(艹卓)化合物，研究了它们的合成反应条件，发现其为动力学控制产物.生物活性研究表明，目标化合物对真菌和细菌都有明显的抑制作用，尤其是对新生隐球菌和大肠杆菌有突出的抑制效果.
关键词: 1,5-苯并硫氮杂(艹卓), 动力学控制产物, 热力学控制产物, 抑菌活性
By introducing N,N-dimethylformamido into 1,5-benzothiazepine, 6 compounds of 2-substituted-phenyl-3-(N,N-dimethylformamido)-4-methyl-1,5-benzothiazepine 3a～3f were designed and synthesized, Studies on the synthesis conditions of 3a～3f revealed that 3a～3f were dynamic control products. 3a～3f had obvious inhibitory effect on fungi and bacteria especially for Cryptococcus neoformans and Escherichia coli.
Key words: 1,5-benzothiazepine, dynamic control product, thermodynamic control product, antimicrobical activity
PDF全文下载地址:
点我下载PDF
