摘要
哌嗪及其衍生物作为药物合成中的重要中间体,显示出了较好的药理活性。本论文以哌嗪为先导化合物,在其N-1位和N-4位分别导入不同种类的氨基酸,10种新型哌嗪衍生物被设计、合成。通过红外光谱、核磁共振氢谱对重要化合物进行结构表征。对所合成的化合物进行了抗菌活性研究。其结果显示化合物P-2,P-4a,P-4b,P-5a和P-5b对金黄色葡萄球菌(Staphylococcus aureus)具有一定的抑制作用,而P-2,P-4a和P-5a对野生型大肠杆菌(Escherichia coli)具有一定的抑制作用。
Piperazine is an important intermediate in drug synthesis, the piperazine derivatives exhibit preferable pharmacological activity. A series of ten novel piperazine derivatives were designed and synthesized through introduction different amino acid moieties in N-1 and N-4 position. Structures of all target compounds were characterized by IR and 1H NMR. Afterwards, the target products were studied by the anti-inflammatory activity. The results indicated that compounds P-2, P-4a, P-4b, P-Sa and P-Sb have some anti-inflammatory activities on Staphylococcus aureus, and compounds P-2, P-4a and P-Sa have some anti-inflammatory activities on Escherichia coli.
出处
《大连大学学报》
2016年第6期49-53,共5页
Journal of Dalian University
基金
国家自然科学基金项目(21102067)
关键词
哌嗪
氨基酸
合成
抑菌活性
piperazine
amino acid
synthesis
anti-inflammatory activity
