Synthesis And Property Of Metal-sensitive And Multi-nuclear MRI Contrast Agents With1,2,3-triazole

In recent two decades, Magnetic resonance imaging (MRI) has become one of themost advanced clinical diagnosis techniques because of its non-invasive ability and highspatial resolution. And as the most effective means of enhance image, MRI contrastagents also have been get rapid development. Metal-sensitive MRI contrast agents andmulti-nuclear MRI contrast agents has become hotspot in recent years because of itsunique advantages. With the development of Click Chemistry, the1,2,3-triazoles havebeen received more attention which have unique chemical properties and medicinal worth.As an effective bridge group, the1,2,3-triazole ring can effectively improve theantimicrobial property of MRI contrast agents.Based on this idea, four Gd(Ⅲ) complexes (A, B, C, D) which are new type, lowtoxicity were designed and synthesized based on Click reaction. These four Gd(Ⅲ)complexes were characterized. And we also study the relaxivity, acute toxicity and imagequality.The organization of the main work is as follows:(1) the research progress of MRIcontrast agent has been reviewed, and one of the most challenging areas of MRI contrastagent research at present is the development of metal-sensitive MRI contrast agents andmulti-nuclear MRI contrast agents.(2) Four four Gd(Ⅲ) complexes (A, B, C, D) havebeen synthesized by using monoethanolamine, diethanol amine, triethanolamine andDTPA as starting materials;(3) study these four four Gd(Ⅲ) complexes’ relaxivity, acutetoxicity and image quality, and the results show that: the relaxivity of MRI contrastagents A, B, C, D respectively is10.5Lmmol-1s-1,9.24Lmmol-1s-1,13.13Lmmol-1s-1,23.87Lmmol-1s-1, which are much higher than the clinical MRI contrastagents-Magnevist. Contrast agents A and contrast agents B is sensitive to metal.Two-nuclear MRI contrast agents C and three-nuclear MRI contrast agents D have quitehigh relaxivity because of more globular structure, slowing rotation and more coordination number of water molecules; MRI contrast agents A, B, C, D have smallacute toxicity; Contrast agent B and contrast agents D get good imaging effect.