Chin. J. Org. Chem. ›› 2019, Vol. 39 ›› Issue (3): 778-785.DOI: 10.6023/cjoc201808005 Previous Articles     Next Articles



孙宏顺a,b, 周进a,b, 李玉龙a, 蒋蕻a, 张艳c, 王建强b, 郭成b, 沈临江b,d   

  1. a 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;
    b 南京工业大学化学与分子工程学院 南京 211816;
    c 盐城工业职业技术学院纺织服装学院 盐城 224005;
    d 南京工业大学数理科学学院 南京 211816
  • 收稿日期:2018-08-07 修回日期:2018-09-30 发布日期:2018-10-26
  • 通讯作者: 孙宏顺
  • 基金资助:


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

Sun Hongshuna,b, Zhou Jina,b, Li Yulonga, Jiang Honga, Zhang Yanc, Wang Jianqiangb, Guo Chengb, Shen Linjiangb,d   

  1. a Targeted Magnetic Resonance Imaging Contrast Agents Laboratory of Jiangsu Province, Nanjing Polytechnic Institute, Nanjing 210048;
    b College of Chemistry and Molecular Engineering, Nanjing Tech University, Nanjing 211816;
    c College of Textiles and Clothing, Yancheng Vocational Institute of Industry Technology, Yancheng 224005;
    d School of Physical and Mathematical Sciences, Nanjing Tech University, Nanjing 211816
  • Received:2018-08-07 Revised:2018-09-30 Published:2018-10-26
  • Contact: 10.6023/cjoc201808005
  • Supported by:

    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 and the Qing Lan Project of Jiangsu Province.

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.

Key words: magnetic resonance imaging (MRI), contrast agents, liver-target, DOTA-hydrazide, gadolinium, synthesis