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新型二茂铁基喹喔啉哌嗪的合成及其抗疟活性研究
Synthesis of Novel Ferrocenyl Quinoxaline Piperazines and Their Relevant Antimalarial Activities
【摘要】 以二茂铁甲醛为起始原料,经过6步反应合成得到新型的二茂铁吡咯并[1,2-α]喹喔啉哌嗪类衍生物1a-h.产物针对恶性疟原虫FcB1,K1,F32等菌株进行了体外抑制活性实验.实验结果表明,新合成的化合物具有一定的抗疟活性,其中芳环上4-位硝基取代的化合物1h体外抗疟活性最优.本工作为进一步研究具有更好活性的抗疟药物打下一定的基础.
【Abstract】 A series of novel ferrocenyl-substituted pyrrolo[1,2-α]quinoxaline piperazines 1a-h were synthesized from ferrocene-carboxaldehyde by six-step reactions.All of the compounds were screened for their antimalarial activities against plasmodium falciparum FcB1,K1,F32 strains.The results revealed that compounds 1 exhibited some inhibitory activities against the plasmodium falciparum strains.Among them,nitro substituted 1h was best.This work laid a foundation for further study of new antimalarial drugs.
【关键词】 二茂铁基;
喹喔啉;
抗疟活性;
恶性疟原虫;
【Key words】 ferrocenyl; quinoxaline; antimalarial activity; plasmodium falciparum;
【Key words】 ferrocenyl; quinoxaline; antimalarial activity; plasmodium falciparum;
【基金】 湖南省自然科学基金资助项目(11JJ5008)
- 【文献出处】 湖南师范大学自然科学学报 ,Journal of Natural Science of Hunan Normal University , 编辑部邮箱 ,2013年04期
- 【分类号】TQ463
- 【被引频次】4
- 【下载频次】77