一类基于1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸-酰肼结构的新型含钆磁共振对比剂的设计、合成及性能表征（英文）  

Design, Synthesis and Evaluation of Novel Gd-Based 1,4,7,10-Tetraazacyclododecan-N,N’,N,N’-tetraacetic Acid-Hydrazide Derived Contrast Agents for Magnetic Resonance Imaging

作　　者：孙宏顺 周进 李玉龙 蒋蕻 张艳[3] 王建强 郭成 沈临江 Sun Hongshun;Zhou Jina;Li Yulong;Jiang Hong;Zhang Yan;Wang Jianqiang;Guo Cheng;Shen Linjiang(Targeted Magnetic Resonance Imaging Contrast Agents Laboratory of Jiangsu Province,Nanjing Polytechnic Institute,Nanjing 210048;College of Chemistry and Molecular Engineering,Nanjing Tech University,Nanjing 211816;College of Textiles and Clothing,Yancheng Vocational Institute of Industry Technology,Yancheng 224005;School of Physical and Mathematical Sciences,Nanjing Tech University,Nanjing 211816)

机构地区：[1]南京科技职业学院江苏省磁共振靶向显像剂工程实验室,南京210048 [2]南京工业大学化学与分子工程学院,南京211816 [3]盐城工业职业技术学院纺织服装学院,盐城224005 [4]南京工业大学数理科学学院,南京211816

出　　处：《有机化学》2019年第3期778-785,共8页Chinese Journal of Organic Chemistry

基　　金：Project supported by the Natural Science Foundation of Jiangsu Province(No.BK20181486);the Natural Science Foundation of the Jiangsu Higher Education Institutions(Nos.17KJB320001,16KJB540006);the Overseas Training Program for Excellent Young Teachers and Principals of Jiangsu Province;the Qing Lan Project of Jiangsu Province~~

摘　　要：磁共振成像技术被广泛应用于诊断医学和软组织成像,而磁共振对比剂有助于提高成像对比度.报道了一类共十二种基于钆-1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸(DOTA)-酰肼结构的新型磁共振对比剂的设计、合成及性能表征. 0.5 T 磁场下测得的弛豫率结果显示,对比剂 5d、5h 和 5l 的纵向弛豫率优于临床使用对比剂 Gd-DOTA,分别达到4.67、4.85 和 5.33 L·mmol^-1·s^-1.进一步动物活体体内肝靶向磁共振成像研究显示,对比剂 5d 具有作为肝靶向磁共振对比剂的应用潜力.Magnetic resonance imaging (MRI) is widely used in diagnostic medicine and soft tissue imaging. Contrast agents (CAs) can improve the specificity of MRI enhancement. Herein, the design, synthesis and characterization of twelve novel Gd-based 1,4,7,10-tetraazacyclododecan-N,N',N,N'-tetraacetic acid (DOTA)-hydrazide derived contrast agents for MRI were reported. Among of them, 5d, 5h and 5l exhibit higher longitudinal relaxivities than the clinical Gd-DOTA at 0.5 T. The relaxivities r1 of 5d, 5h and 5l are 4.67, 4.85 and 5.33 L·mmol^-1·s^-1 respectively. In vivo liver-target MRI shows that the potential of complex 5d was used as a novel liver-target contrast agent for MRI.

关 键 词：磁共振成像 对比剂 肝靶向 DOTA-酰肼 钆 合成 

分 类 号：TQ463[化学工程—制药化工]