二乙三胺五乙酸二氢吡啶衍生物的合成及Gd(Ⅲ),Fe(Ⅲ),Mn(Ⅱ)配合物的弛豫性能研究

Synthesis, Relaxivity of Gd(Ⅲ), Fe(Ⅲ) and Mn(Ⅱ) Complexes with Dihydropyridine Derivatives of Diethylenetriaminepentaacetic Acid

用二乙三胺五乙酸 ( DTPA)酸酐与二氢吡啶类化合物反应 ,合成了 4种新型的含二氢吡啶基的二乙三胺五乙酸非离子型配体 ,并进一步合成了其 Gd( ) ,Fe( ) ,Mn( )的顺磁性金属配合物 .配体和配合物的结构用 IR,1 H NMR及元素分析表征 .研究了配合物的体外弛豫性能 ,结果表明 ,Fe( )和 Mn( )配合物弛豫效率 R1 低于 Gd( )配合物的 R1 ,Gd( )配合物的弛豫效率较高 ,具有作为 MRI造影剂的条件 .

Four novel ligands of DTPA-dihydropyridine derivatives which were designed for magnetic resonance imaging contrast agents were synthesized by the reaction between DTPA-dianhydride and 4-aniline-1,4-dihydropyridines. Their complexes of gadolinium, manganese and iron were prepared. Spin-lattice relaxivities(t 1) of the complexes was investigated. The results showed that all the complexes have relaxation effects on the protons in surrounding water molecules. The Gd(Ⅲ) complexes have higher relaxivities than those of Fe(Ⅲ) and Mn(Ⅱ) complexes. The NMR t 1 relaxivities(R 1) of Gd(Ⅲ)DTPA-dihydropyridines complexes are 5.50, 5.58, 5.20 and 5.49 L·mmol -1·s -1, which are higher than that of their parent complex, GdDTPA 2-. That indicating that the Gd(Ⅲ) complex possesses the precondition to be the contrast agents for magnetic resonance imaging.