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放射性核素乏氧显像已成为肿瘤诊断、治疗中的重要手段。有相当数量的硝基咪唑类化合物作为乏氧显像剂用于临床前及临床研究。如何设计出理想的显像剂结构正逐步成为新型显像剂开发的关键。显像剂中硝基咪唑的类型和数量、连接基团的结构和化合物手性等都直接影响显像效果;而显像剂整体的性质如单电子还原电势、油水分配系数及药物动力学特征也是关键因素。本文通过探讨影响硝基咪唑类化合物显像效果的因素,为显像剂的设计提供一定的思路。
Radionuclide hypoxia imaging has become an important tool in the diagnosis and treatment of tumors. A considerable amount of nitroimidazoles are used as hypoxic imaging agents in preclinical and clinical studies. How to design an ideal imaging agent structure is gradually becoming the key to the development of new imaging agents. The type and amount of nitroimidazole in the imaging agent, the structure of the linker and the chirality of the compound all have a direct effect on the imaging effect. The properties of the imaging agent such as the single electron reduction potential, the oil-water partition coefficient and the pharmacokinetic characteristics Is also a key factor. In this paper, by exploring the factors that affect the imaging effect of nitroimidazoles, we can provide some ideas for the design of imaging agents.