首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Influence of trans-1,2-diaminocyclohexane structure and mixed carboxylic/phosphonic group combinations on samarium-153 chelation capacity and stability.
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Influence of trans-1,2-diaminocyclohexane structure and mixed carboxylic/phosphonic group combinations on samarium-153 chelation capacity and stability.

机译:反式1,2-二氨基环己烷的结构和羧基/膦酸混合基团对combinations153螯合能力和稳定性的影响。

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摘要

A simple procedure was developed to compare chelating agents for (153)Sm complexes as a preliminary step to synthesise bifunctional analogues. Several variables affecting the efficiency of complex stability were investigated, such as the pre-organisation concept, cavity size, and the nature of coordination sites. Four semi-rigid agents incorporating carboxylic and/or phosphonic groupings fixed at trans-1,2-diaminocyclohexane were evaluated for their (153)Sm chelation properties, and competition studies were performed. Data on the stability of the best chelating agent compound 3: trans-cyclohexane-1,2-bis(aminomethylphosphonic)-N,N'-bis(ethyl-2-iminodia cetic acid) in human serum are presented.
机译:开发了一种简单的程序来比较(153)Sm络合物的螯合剂,作为合成双功能类似物的第一步。研究了影响复杂稳定性效率的几个变量,例如组织前的概念,空腔的大小以及配位点的性质。评估了四个固定在反式1,2-二氨基环己烷上的羧基和/或膦酸基团的半刚性试剂的(153)Sm螯合性能,并进行了竞争研究。给出了关于最佳螯合剂化合物3的稳定性的数据:反式环己烷-1,2-双(氨基甲基膦酸)-N,N'-双(乙基-2-亚氨基二乙酸)在人血清中的稳定性。

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