化学交换饱和转移MRI对比剂的合成与性质研究  

Synthesis and Properties of Chemical Exchange Saturation Transfer MRI Contrast Agents

作　　者：李娜梅 薄少伟 LI Na-mei;BO Shao-wei(Department of Pharmacy,Affiliated Guangdong Second Provincial General Hospital of Jinan University,Guangdong Guangzhou 510317;Department of Nuclear Medicine,Affiliated Guangdong Second Provincial General Hospital of Jinan University,Guangdong Guangzhou 510317,China)

机构地区：[1]暨南大学附属广东省第二人民医院药学部,广东广州510317 [2]暨南大学附属广东省第二人民医院核医学科,广东广州510317

出　　处：《广州化工》2024年第15期32-34,41,共4页GuangZhou Chemical Industry

基　　金：广东省基础与应用基础研究基金项目(No:2021A1515111129)。

摘　　要：化学交换饱和转移(CEST)磁共振成像(MRI)是一种新型的分子成像技术,它能够实现对体内低浓度的特定分子进行成像,被广泛应用于肿瘤疾病、神经系统疾病、心血管疾病、肾脏疾病等的诊断和评估。然而,许多现有的CEST对比剂由于其可交换质子和水之间的化学位移较小(≤4 ppm)而限制了其成像灵敏度,因此,迫切需要开发具有较大化学位移的CEST对比剂。本研究中,我们在酰肼化合物结构的基础上开发了一系列基于酰腙结构的CEST对比剂并对其性质进行研究,结果发现这类化合物表现出很好的水溶性,并且其距离水信号的化学位移范围为5.2~6.8 ppm,具有较好的CEST成像效果,表明酰腙键的构建是一种优良的CEST对比剂设计方法。该类化合物的发现扩大了CEST对比剂的化合物库,有利于进一步推动CEST MRI的应用。Chemical exchange saturation transfer(CEST) MRI is a novel molecular imaging technique that can visualize specific molecules in vivo with low concentration.CEST MRI is widely applied in the diagnosis and assessment of cancer,neurological diseases,cardiovascular diseases and kidney diseases.However,many existing CEST contrast agents exhibit sensitivity limitation due to small chemical shifts(≤4 ppm) between their exchangeable protons and water.Therefore,there is an urgent need to develop CEST contrast agents with large chemical shifts.A series of acyl-hydrazone CEST contrast agents based on acyl-hydrazides were developed and their properties were studied.These agents showed good water solubility and exhibited chemical shifts ranging from 5.2 ppm to 6.8 ppm,providing better CEST imaging effect.This indicated that the construction of acyl-hydrazone bonds was an excellent method for designing CEST contrast agents.Discovery of these compounds can expand the compound library of CEST contrast agents,which promoted the application of CEST MRI.

关 键 词：化学交换饱和转移 磁共振成像 酰腙 对比剂 

分 类 号：R914.5[医药卫生—药物化学]