Manganese Complex of Ethylenediaminetetraacetic Acid (EDTA)–Benzothiazole Aniline (BTA) Conjugate as a Potential Liver-Targeting MRI Contrast Agent,Journal of Medicinal Chemistry

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Manganese Complex of Ethylenediaminetetraacetic Acid (EDTA)–Benzothiazole Aniline (BTA) Conjugate as a Potential Liver-Targeting MRI Contrast Agent
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-03-22 00:00:00 , DOI: 10.1021/acs.jmedchem.6b01799
Md. Kamrul Islam , Soyeon Kim , Hee-Kyung Kim , Subin Park , Gang-Ho Lee , Hyo Jeung Kang , Jae-Chang Jung , Joon-Suk Park ₁ , Tae-Jeong Kim , Yongmin Chang

Affiliation

A novel manganese(II) complex based on an ethylenediaminetetraacetic acid (EDTA) coordination cage bearing a benzothiazole aniline (BTA) moiety (Mn-EDTA-BTA) was designed and synthesized for use as a liver-specific MRI contrast agent with high chelation stability. In addition to forming a hydrophilic, stable complex with Mn²⁺, this new Mn chelate was rapidly taken up by liver hepatocytes and excreted by the kidneys and biliary system. The kinetic inertness and R₁ relaxivity of the complex were much higher than those of mangafodipir trisodium (MnDPDP), a clinically approved liver-specific MRI contrast agent. The diagnostic utility of this new Mn complex in MRI was demonstrated by high-sensitivity tumor detection in an animal model of liver cancer.

中文翻译：

乙二胺四乙酸（EDTA）-苯并噻唑苯胺（BTA）的锰配合物可作为靶向肝脏的MRI造影剂

设计并合成了一种新的基于乙二胺四乙酸（EDTA）配合笼并带有苯并噻唑苯胺（BTA）部分（Mn-EDTA-BTA）的锰（II）配合物，用作具有高螯合稳定性的肝脏特异性MRI造影剂。除了与Mn ²⁺形成亲水稳定的络合物外，这种新的Mn螯合物还被肝脏的肝细胞迅速吸收，并被肾脏和胆汁系统排泄。该复合物的动力学惰性和R ₁弛豫性远远高于临床批准的肝脏特异性MRI造影剂锰福地吡三钠（MnDPDP）。通过在肝癌动物模型中高灵敏度肿瘤检测证明了这种新的Mn络合物在MRI中的诊断效用。

更新日期：2017-03-22

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