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新型哌嗪类苯乙酮衍生物的合成及生物活性 被引量：3

Synthesis and biological activities of novel hybrid compounds based on piperazines and acetophenones
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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8.33μg/mL,1.04μg/mL),可作为先导化合物进一步研究。 A series of novel hybrid derivatives based onstructures were characterized by H NMR and 3C NMR.acetophenones and piperazines were synthesized; and theThe 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 antibacterialactivity against Pseudomonas aeruginosa （ MIC = 8.33 μg/mL） and Escherichia coli （ MIC = 1.04 μg/mL）. Com-pound Ⅱ1 could be a lead compound for further structural modifications and biological evaluation.
作者 毛泽伟 万春平 郑喜 姜圆 饶高雄
机构地区 云南中医学院药学院 云南中医学院第一附属医院中心实验室
出处 《中国药科大学学报》 CAS CSCD 北大核心 2014年第5期517-521,共5页 Journal of China Pharmaceutical University
基金 云南省应用基础研究资助项目(No.2013FZ088)~~
关键词 哌嗪 苯乙酮 衍生物 合成 生物活性 piperazine acetophenone derivatives synthesis biological activity
分类号 R914.5 [医药卫生—药物化学]
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参考文献15

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二级参考文献10

共引文献18

同被引文献20

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中国药科大学学报
2014年 第5期

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