Structure-Relaxivity Relationships of Serum Albumin Targeted MRI Probes Based on a Single Amino Acid Gd Complex

被引：29

作者：

Boros, Eszter ^{[1
]}

Caravan, Peter ^{[1
]}

机构：

[1] Harvard Univ, Massachusetts Gen Hosp, Athinoula A Martinos Ctr Biomed Imaging, Dept Radiol,Med Sch, Charlestown, MA 02129 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 56卷 / 04期

基金：

瑞士国家科学基金会;

关键词：

CONTRAST AGENTS; PHYSICOCHEMICAL CHARACTERIZATION; GADOLINIUM; BINDING; ENHANCEMENT; MS-325; MEDIA;

D O I：

10.1021/jm4000177

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The Gd(III) complex of DO3A-N-alpha-aminopropionate, Gd(DOTAla), was used to generate a small library of putative MRI probes targeted to human serum albumin (HSA). Ten compounds were synthesized via multistep organic synthesis, and the corresponding Gd complexes were investigated for their affinity to HSA, lipophilicity, and relaxivity in the absence and presence of HSA. Negative charge and moderate lipophilicity correlate with increased HSA affinity and relaxivity

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收藏

页码：1782 / 1786

页数：5

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