双分子取代苯酚氨羧酸螯合剂对放射性钍促排活性的构效关系

Structure activity relationship study of chelating agents of double molecular substituted phenols amino carboxylic acid for decorporated radiothorium\

目的对已合成的１５个双分子取代苯酚氨羧酸螯合剂经动物实验观察对２３４Ｔｈ的促排活性，以探讨化学结构与促排活性的构效关系。方法以大鼠尿、粪中２３４Ｔｈ排出量的增高，组织（肝、骨）中蓄积量的降低与对照组比较作为评价指标。结果１５个螯合剂中除４个外均显示不同程度的促排活性，其中有３个其尿、粪中２３４Ｔｈ的排出量达６０％～７０％，肝、骨中２３４Ｔｈ的蓄积量明显降低。结论取代基中邻苯二酚类的促排活性为最好，为本实验之冠，间苯二酚的活性最差，对苯二酚居中。

Objective\ To study the effects of synthesized chelating agents of double molecular substituted phenols amino carboxylic acid on decorporated radiothorium in rats and to explore the relationship between their chemical structure and bioactivity. Methods Chelating agents could increase the excretion of 234 Th in urine and feces and decrease its retention in liver and skeleton of rats as compared with the control group. Results The chelating agents showed different bioactivity for decorporated thorium except 4 agents.Three of them could increase excretion of 234 Th in urine and feces by 60 70% and decrease markedly retention of 234 Th in liver and skeleton. Conclusion Chelating agents of the catechol series have been proved to be superior to others.They are the best ones while the resorcinol is the worst and hydroquinone is ranked between them.