锕系元素的螯合药物——Ⅹ.新型镅促排药物的研究

SPECIFIC SEQUESTERING AGENTS FOR THE ACTINIDES Ⅹ.STUDY OF THE DECORPORATION DRUGS FOR AMERICIUM

设计、合成了14个多氨基多羧基酚类螯合剂,其中10个是未见文献报告的新化合物。对10个螯合剂进行^(241)Am促排药效的研究,动物实验表明,在50μmol/kg剂量下有7个对肝镅有明显促排效果,整合剂Va对肝镅、骨镅和肾镅均有明显促排作用。

In this article,ten new and four known polyaminocarboxy- licphenolic sequestering agents have been synthesized.The result of animal screen- ing of ten of these sequestering agents indicates:six of all,at a dose of 50μmol/kg can excrete liver Am·Va(N,N′-di(2-hydroxybenzyl)-diethylenetriamine-N^1, N^4,N^7-triacetic acid)is the mest effective,it can excrete liver Am,skele- ten Am and kidney Am.But all are less effective than DTPA.The structure- activity relationship has been discussed,ligand with more aminocarboxylic acid groups showed a better result than the ligand with more phenolic groups.