新型哌嗪类苯乙酮衍生物的合成及生物活性

Synthesis and biological activities of novel hybrid compounds based on piperazines and acetophenones

摘要: 在苯乙酮的苯环部分进行结构修饰，通过引入哌嗪基团，设计并合成了12个未见文献报道的哌嗪类苯乙酮新化合物，其结构经¹H NMR和¹³C NMR确证。分别采用MTT法和滤纸片扩散法测试目标化合物的细胞毒活性和抗菌活性。结果表明，化合物 Ⅱ1 不仅表现出一定的细胞毒活性，还对铜绿假甲胞菌和大肠埃希菌有较强的抑制作用(MIC分别为8.33 μg/mL，1.04 μg/mL)，可作为先导化合物进一步研究。

Abstract: A series of novel hybrid derivatives based on acetophenones and piperazines were synthesized; and the structures were characterized by ¹H NMR and ¹³C NMR. The result of in vitro assays indicated that compound Ⅱ1 was most potent against 3 strains of human tumor cell lines(HeLa, A549 and H1975), with moderate antibacterial activity against Pseudomonas aeruginosa(MIC=8. 33 μg/mL)and Escherichia coli(MIC=1. 04 μg/mL). Compound Ⅱ1 could be a lead compound for further structural modifications and biological evaluation.