论文部分内容阅读
通过酰化反应将一种新型杂环化合物2-肼基-5-甲基-10bH-1,3,4-噻二唑[3,2-c]喹唑啉-6-10b-羧酸化合物(HC)引入到二乙三胺五乙酸(DTPA)结构中得到新型DTPA双酰胺杂环配体(DTPA-HC),再与Gd3+,Mn2+以及Fe3+配位得到相应的功能配合物作为潜在的磁共振成像造影剂。其结构通过FTIR、元素分析、TG进行表征。配合物的纵向弛豫率(longitudinal relaxivity,r1)结果表明,Gd基配合物的r1〔13.20 L/(mmol.s)〕和Mn基配合物的r1〔12.11 L/(mmol.s)〕远远大于商业化医用的磁共振成像造影剂Gd-DTPA〔r1=3.620 L/(mmol.s)〕。通过等温滴定微量热法(isothermal titration calorimetry,ITC)测定了各配合物与牛血清白蛋白(BSA)相互作用的热力学参数,结果得到Gd基配合物与BSA作用的结合常数Ka(1.171×106)大于Mn基(2.913×105)和Fe基(4.042×104)配合物与BSA的结合常数。
A novel heterocyclic compound, 2-hydrazinyl-5-methyl-10bH-1,3,4- thiadiazolo [3,2-c] quinazoline-6-10b-carboxylic acid compound (DTPA) was introduced into the structure of diethylenetriaminepentaacetic acid (DTPA) to form the corresponding functional complex with Gd3 +, Mn2 + and Fe3 + as the potential magnetic Resonance imaging contrast agent. Its structure was characterized by FTIR, elemental analysis and TG. The longitudinal relaxivity (r1) of the complex showed that r1 [13.20 L / (mmol · s)] of the Gd-based complex and r1 [12.11 L / (mmol · s)] of the Mn-based complex were far Is much larger than the commercially available magnetic resonance imaging contrast agent Gd-DTPA [r1 = 3.620 L / (mmol.s)]. The thermodynamic parameters of each complex with bovine serum albumin (BSA) were determined by isothermal titration calorimetry (ITC). The results showed that the binding constant of the Gd-based complex with BSA was 1.171 × 106, Is larger than the binding constant of Mn (2.913 × 10 5) and Fe (4.042 × 10 4) complexes with BSA.