文献类型：期刊文献

中文题名：基于季胺基修饰的核磁共振成像造影剂的合成

英文题名：Synthesis of Magnetic Resonance Imaging Contrast Agent with Tethered Quaternary Ammonium Group

作者：王伟[1];汤伟军[2];郝士婧[1];陈莹莹[1];胡爱国[1]

机构：[1]华东理工大学材料科学与工程学院,上海市先进聚合物材料重点实验室,上海200237;[2]复旦大学附属华山医院放射科,上海200040

年份：2013

卷号：39

期号：5

起止页码：523

中文期刊名：华东理工大学学报（自然科学版）

外文期刊名：Journal of East China University of Science and Technology

收录：CSTPCD;;Scopus;北大核心:【北大核心2011】；CSCD:【CSCD2013_2014】；

基金：国家自然科学基金(21274042)

语种：中文

中文关键词：核磁共振成像;造影剂;季胺基;长链烷烃

外文关键词：MRI; contrast agent; quaternary ammonium group; long alkane chain

摘要：利用季胺基团具有高水溶性的特点,合成了一种水溶性良好且带有长烷烃链的核磁共振成像造影剂。通过在1,4,7,10-四氮杂环十二烷(cyclen)的骨架碳原子上引入季胺基团,并分别对4个仲氨基进行亲电取代,得到具有季胺基侧链的多齿配体;在不影响对钆(Ⅲ)离子的络合能力的同时,提高了配合物的弛豫率,并赋予其良好的水溶性。长烷烃链和季胺基团的同时引入为该类配合物的进一步功能化提供了可能性。
Benefited with the high water solubility of quaternary ammonium group, a magnetic resonance imaging （MRI） contrast agent with tethered quaternary ammonium group linked by long alkyl chain was synthesized. The quaternary ammonium group was introduced in the skeleton of 1,4,7,10- tetraazacyclododecane （cyclen）, and four secondary amino groups in cyclen were functionalized with carboxymethyl groups, forming a polychelating ligand with a quaternary ammonium side chain. Without affecting the conjugation ability, this ligand forms stable Gd（III） complex showing higher relaxivity than Gd（III）-DOTA. With both quaternary ammonium group and long alkyl chain installed in the same molecule, further functionalization or modification to achieve high performance MRI contrast agents is promising.