铀促排药物研究:Ⅳ,N,N′-双-[N-羧甲基-(2,3-二羟基-5-甲氧羰基苄胺乙酰基]-α,ω-二胺的合成

STUDIES ON URANIUM MOBILIZATION AGENTS Ⅳ. SYNTHESIS OF N, N'-BIS-[N-CARBOXYMETHYL-(2, 3-DIHYDROXY-5-CARBOMETHOXY) BENZYLAMINOACETYL]-α, ω-DIAMINES

随着核工业的迅速发展,核燃料铀对人类构成了一种潜在威脅。铀在人体脏器内的沉积不但引起损伤,并能诱发肿瘤。关于铀的促排解毒药物,虽有一些报道,但未见在临床应用。作者等曾合成了多个系列新的膦酸类和邻苯二酚类双取代或单取代胺羧酰胺螫合剂,动物试验结果表明其中的大多数排铀效果显著,尤其是邻苯二酚类单取代胺羧酰胺(Ⅰ)中,若干化合物排铀效果远远超过文献报道较多的钛铁试剂和Phosphicine。

In continuation of searching for effective antidotes against uranium intoxication, a series of N, N′-bis-[N-carboxymethyl-(2,3-dihydroxy-5-carbomethoxy) benzylaminoacetyl]-α, ω-diamines was synthesized by reacting 2, 3-dihydroxy-5-carbomethoxybenzylamine diacetic acid with diamines of different chain lengths. Their effects on the elimination of uranyl nitrate from rats were tested. Most of them were found to be more effective than the reported uranium chelating agents as Tiron and Phosphicine and compound Ⅱa was shown to be the most promising. The results of pharmacological studies will be published elsewhere.