哌嗪的氨基酸缀合物的合成、表征及抑菌活性研究

Synthesis and Characterization of the Amino Acids Conjugates of Piperazine, and the Study on the Anti-inflammatory Activity

哌嗪是化工生产的常用化合物,也是重要的医药中间体。近些年来,哌嗪类衍生物作为药物的研发引起了人们的广泛关注。本文以哌嗪为起始原料,将4种氨基被保护的氨基酸导入哌嗪的N-1和N-4位,再脱去保护基,合成了8种哌嗪的氨基酸缀合物,并通过IR和1H NMR对所合成的氨基酸缀合物进行了结构表征。然后对目标产物进行了野生型大肠杆菌(Escherichia coli)和金黄色葡萄球菌(Staphylococcus aureus)抑菌活性测试。结果表明化合物PP-1a、PP-2a、PP-1b、PP-2b、PP-1c、PP-2c、PP-2d对Staphylococcus aureus具有一定的抑菌效果并且抑菌作用随化合物浓度的升高而增强。

Piperazine is not only the commonly used compound, but also the important pharmaceutical intermediate. In recent years, piperazine derivatives as drug development have aroused widespread concern. Piperazine is as the starting material, the four amino acids which amino group was protected were introduced into N-1 and N-4 position of the piperazine, and then removing the protecting group, eight amino acids conjugates were synthesized. The conjugates were characterized by IR and 1H NMR. Afterwards, the target products were studied by the anti-inflammatory activity of wild-type Escherichia coli and Staphylococcus aureus. The results showed that compounds PP-1a, PP-2a, PP-1b, PP-2b, PP-1c, PP-2c, and PP-2d have some anti-inflammatory activities on Staphylococcus aureus and the anti-inflammatory activities increased with the concentration of the compound strengthening.