一类新的羟基苯二磺酰苯胺类化合物的合成及其杀虫活性  

SYNTHESIS AND INSECTICIDAL ACTIVITY OF THE NOVEL HYDROXYLBENZENEDISULFONANILIDES COMPOUNDS

作　　者：石玉[1] 江雅新[1] 牛雪平[1] 赵军[1] 王小晶[1] 新民[1] 

机构地区：[1]内蒙古大学化学化工学院,内蒙古呼和浩特010021

出　　处：《药学学报》2002年第9期700-704,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目( 1972 97)

摘　　要：目的　合成并筛选出杀虫活性较好的新型抗肝片吸虫病化合物。方法　分别以邻 (间、对 )氯苯酚为原料 ,通过磺酰化和亲核取代反应合成了 1 4种羟基苯二磺酰苯胺类化合物 ;通过元素分析、红外光谱及核磁共振氢谱对合成的 1 4种新型抗肝片吸虫病化合物羟基苯二磺酰苯胺类化合物 (1～ 1 4 )的结构进行了表征 ,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　所合成的大部分羟基苯二磺酰苯胺类化合物均具有较好的解偶联活性 ,其中 3 ,5 ,6 ,9的杀虫活性最好。结论化合物 3 ,5 ,6 。AIM To synthesize novel derivatives of hydroxylbenzenedisulfonanilide with high inse cticidal activity against the Fasciola hepatica . METHODS o ( m , p ) Chlorphenol were used to synthesize the title compoun ds by sulphon ation and nucleiphilic substitution reaction. The uncoupling activity (insectic idal activity) of these compounds were tested by determining the influence on mi tochondrial respiration control ratio (RCR) and the variation of inorganic phosp hate in oxidative phosphorylation (ΔPi). RESULTS Compounds 1～14 are new compounds. The structures of the c ompounds were determined by IR, HNMR and elemental analysis. Most new compounds have relatively high uncoupling activities, especially compounds 3, 5, 6 and 9. CONCLUSION Compounds 3, 5, 6 and 9 will become novel fasciolicides and are worth further studying.

关 键 词：肝片吸虫 羟基苯二磺酰苯胺类化合物 杀虫活性 合成方法 化学结构 

分 类 号：R532.2[医药卫生—内科学] R978.6[医药卫生—临床医学]