Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (7): 1779-1785.DOI: 10.6023/cjoc201801044 Previous Articles     Next Articles



孙宏顺a,b, 李玉龙b, 蒋蕻b, 郭成a, 沈临江a,c   

  1. a 南京工业大学 化学与分子工程学院 南京 211816;
    b 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;
    c 南京工业大学 数理科学学院 南京 211816
  • 收稿日期:2018-01-29 修回日期:2018-03-04 发布日期:2018-03-29
  • 通讯作者: 沈临江
  • 基金资助:


Two Binuclear Nonionic Magnetic Resonance Contrast Agents with High Relaxivity

Sun Hongshuna,b, Li Yulongb, Jiang Hongb, Guo Chenga, Shen Linjianga,c   

  1. a College of Chemistry and Molecular Engineering, Nanjing Tech University, Nanjing 211816;
    b Targeted MRI Contrast Agents Laboratory of Jiangsu Province, Nanjing Polytechnic Institute, Nanjing 210048;
    c School of Physical and Mathematical Sciences, Nanjing Tech University, Nanjing 211816
  • Received:2018-01-29 Revised:2018-03-04 Published:2018-03-29
  • Contact: 10.6023/cjoc201801044
  • Supported by:

    Project supported by the Natural Science Foundation in Jiangsu Province (No. 17KJB320001), the Top-notch Academic Programs Project of Jiangsu Higher Education Institutions (No. PPZY2015B179), the Training Program of Students Innovation and Entrepreneurship in Jiangsu Province (No. 201712920001Y), 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 relaxivity of two novel binuclear nonionic Gd-based DOTA-hydrazide derived MRI contrast agents, (Gd-DOTAH)2-DYMB and (Gd-DOTAH)2-DYMBP are reported. They have improved longitudinal relaxivity values of 11.4 and 11.7 L·mmol-1·s-1 per molecule or 5.7 and 5.9 L·mmol-1·Gd-1·s-1 at 0.5 T, respectively, which are higher than that of the mononuclear clinical macrocyclic agent Gd-DOTA. And in vitro MRI studies suggest the potential of these two agents as MRI contrast agents in improving the diagnostic sensitivity and accuracy.

Key words: magnetic resonance imaging (MRI), contrast agents, synthesis, relaxivity, DOTA-hydrazide, Gd-DOTA