Chemistry and Synthesis Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD 20850, USA.
Center for Infectious Disease Imaging, Radiology and Imaging Sciences, Clinical Center, National Institutes of Health, Bethesda, MD 20892, USA.
Molecules. 2023 Apr 27;28(9):3773. doi: 10.3390/molecules28093773.
The use of radiolabeled glucose for PET imaging resulted in the most commonly used tracer in the clinic, 2-deoxy-2-[F]fluoroglucose (FDG). More recently, other radiolabeled sugars have been reported for various applications, including imaging tumors and infections. Therefore, in this study, we developed a series of fluorine-18-labeled L-rhamnose derivatives as potential PET tracers of various fungal and bacterial strains. Acetyl-protected triflate precursors of rhamnose were prepared and radiolabeled with fluorine-18 followed by hydrolysis to produce L-deoxy [F]fluororhamnose. The overall radiochemical yield was 7-27% in a 90 min synthesis time with a radiochemical purity of 95%. In vivo biodistribution of the ligands using PET imaging showed that 2-deoxy-2-[F]fluoro-L-rhamnose is stable for at least up to 60 min in mice and eliminated via renal clearance. The tracer also exhibited minimal tissue or skeletal uptake in healthy mice resulting in a low background signal.
放射性标记葡萄糖用于 PET 成像，导致 2-脱氧-2-[F]氟葡萄糖（FDG）成为临床上最常用的示踪剂。最近，其他放射性标记的糖已被报道用于各种应用，包括肿瘤和感染的成像。因此，在这项研究中，我们开发了一系列氟-18 标记的 L-鼠李糖衍生物，作为各种真菌和细菌菌株的潜在 PET 示踪剂。鼠李糖的乙酰保护三氟甲磺酸酯前体被制备并用氟-18 标记，然后水解生成 L-脱氧[F]氟鼠李糖。在 90 分钟的合成时间内，总放射化学收率为 7-27%，放射化学纯度为 95%。使用 PET 成像进行的配体体内生物分布研究表明，2-脱氧-2-[F]氟-L-鼠李糖在小鼠体内至少稳定 60 分钟，并通过肾脏清除。示踪剂在健康小鼠中也表现出最小的组织或骨骼摄取，导致背景信号低。
