新型水杨醛-芳胺席夫碱化合物的合成及生物活性  

Synthesis and biological activity of the novel salicylaldehyde-phenylamine Schiff base compounds

作　　者：赵文岩[1] 牛雪平[2] 张蕊[2] 

机构地区：[1]南开大学环境科学与工程学院,天津300017 [2]内蒙古大学化学化工学院,内蒙古呼和浩特010021

出　　处：《中国药学杂志》2005年第1期63-66,共4页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目 (2 9962 0 0 1)

摘　　要：目的　合成并筛选出生物活性较好的新型抗肝片吸虫病化合物。方法　以水杨醛为原料合成了 15种卤 (硝 )代水杨醛 芳胺席夫碱类化合物 ;通过元素分析、红外光谱及核磁共振氢谱对合成的 15种新化合物进行了表征 ,并测定其对线粒体呼吸控制率的影响以及线粒体呼吸过程无机磷的变化 ,以此对化合物的解偶联活性 (杀虫活性 )进行了评价。结果　所合成的大部分卤代水杨醛 芳胺席夫碱类化合物均有较好的活性 ,其中 4 ,10 ,15的杀虫活性最好。结论　化合物 4 ,10 ,15均有望成为新型的抗肝片吸虫病药物。OBJECTIVE: To synthesize and select novel derivatives of salicylaldehyde-phenylamine Schiff base with high insecticidal activity against the Fascila hepatica. METHODS: Salicylal was used to synthesize the tide compounds by halogenation and nitration reaction. The structures of the compounds were determined by IR, HNMR and elecmental analysis. Meanwhile their uncoupling activity (insectidal activity) was determined with the influence on mitochondrial respiration control ratio (RCR) and the variation of inorganic phosphate in oxidative phosphorylation(ΔPi). RESULTS: Compounds 1 ∼ 15 were new compounds. The results showed that most of them had relatively high uncoupling activities, especially compound 4, 10 and 15. CONCLUSION: Compound 4, 10 and 15 appeared to be potential novel faciolicides and are worth further study.

关 键 词：肝片吸虫 卤(硝)代水杨醛-芳胺席夫碱 杀虫活性 氧化磷酸化 

分 类 号：R916.41[医药卫生—药学] R162.2