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Chinese Journal of Organic Chemistry >

2019 , Vol. 39 >Issue 3: 778 - 785

DOI: https://doi.org/10.6023/cjoc201808005

Articles

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 Hongshun ,
  • Zhou Jin ,
  • Li Yulong ,
  • Jiang Hong ,
  • Zhang Yan ,
  • Wang Jianqiang ,
  • Guo Cheng ,
  • Shen Linjiang
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  • 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 date: 2018-08-07

  Revised date: 2018-09-30

  Online published: 2018-10-26

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.

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Abstract

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

Cite this article

Sun Hongshun , Zhou Jin , Li Yulong , Jiang Hong , Zhang Yan , Wang Jianqiang , Guo Cheng , Shen Linjiang . 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[J]. Chinese Journal of Organic Chemistry, 2019 , 39(3) : 778 -785 . DOI: 10.6023/cjoc201808005

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