卤硝酚类化合物的合成及体外抗螨虫活性研究  

Synthesis and biological activity of novel compounds containing structure of halonitrophenol

作　　者：张海平[1] 牛雪平[1] 石玉[1] 刘迎贵[1] 李哲[1] 

机构地区：[1]内蒙古大学化学化工学院

出　　处：《中国新药杂志》2008年第4期303-307,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金资助项目(29962001,29962004)

摘　　要：目的:合成并筛选生物活性好的抗螨虫化合物,且测试部分化合物抗肝片吸虫的生物活性。方法:以卤硝酚为原料合成了15个新化合物,经元素分析、红外光谱(IR)、核磁共振氢谱(1HNMR)确认结构;测定化合物的体外抗螨活性;测定部分化合物抗肝片吸虫活性。结果和结论:15个化合物均有抗螨活性和氧化磷酸化解偶联活性。1,2,3,4,6,8,13,14等8个化合物具有较好的杀螨药效,特别是化合物2,6,8,13,可驱杀螨虫和肝片吸虫等内外寄生虫。Objective：To synthesize and screen the halonitrophenol compounds with highly insecticidal activity against ectoparasites and fascila hepatica. Methods ： Salicylal was used to synthesize the title compound 1 - 15 by nitration,halogenation and nucleiphilic-substitution reaction. The structures of these compounds were confirmed by elemental analysis, IR and 1^ HNMR spectroscopic evidence. The miticidal activities were tested in vitro. The insecticidal activity of some compounds were determined in mitochondrial respiration control ratio （RCR）. Results and Conclusion ：The compound 1 - 15 were new compounds. Most of them showed higher insecticidal activity, especially compound 2, 6, 8 and 13 also showed the activity against ectoparasites and fascila hepatica.

关 键 词：含卤硝酚结构化合物 合成 杀虫活性 

分 类 号：R978.6[医药卫生—药品] R916.4[医药卫生—药学]