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

doi:10.6023/cjoc201808005

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

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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

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

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 E-mail:njutshs@126.com
基金资助:
江苏省江苏省江苏省江苏省青蓝工程资助项目.

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^a,b, Zhou Jin^a,b, Li Yulong^a, Jiang Hong^a, Zhang Yan^c, Wang Jianqiang^b, Guo Cheng^b, Shen Linjiang^b,d

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 E-mail:njutshs@126.com
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.

1. 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.PDF(4776KB)

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]. Chin. J. Org. Chem., 2019, 39(3): 778-785.

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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

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

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