Synthesis and Evaluation of Novel Norfloxacin Isonitrile 99mTc Complexes as Potential Bacterial Infection Imaging Agents.

Qing Ruan,Si’An Fang,Yuhao Jiang,Junbo Zhang,Xuran Zhang,Qianqian Gan,Di Xiao

doi:10.3390/pharmaceutics13040518

Qing Ruan, Si’An Fang + Show 5 more

Open Access

https://doi.org/10.3390/pharmaceutics13040518

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Journal: Pharmaceutics	Publication Date: Apr 9, 2021
Citations: 4	License type: CC BY 4.0

Affiliation: Beijing Normal University

Abstract

To develop potential technetium-99m single-photon emission computed tomography (SPECT) imaging agents for bacterial infection imaging, the novel norfloxacin isonitrile derivatives CN4NF and CN5NF were synthesized and radiolabeled with a [99mTc][Tc(I)]+ core to obtain [99mTc]Tc-CN4NF and [99mTc]Tc-CN5NF. These compounds were produced in high radiolabeling yields and showed hydrophilicity and good stability in vitro. The bacterial binding assay indicated that [99mTc]Tc-CN4NF and [99mTc]Tc-CN5NF were specific to bacteria. Compared with [99mTc]Tc-CN4NF, biodistribution studies of [99mTc]Tc-CN5NF showed a higher uptake in bacteria-infected tissues than in turpentine-induced abscesses, indicating that [99mTc]Tc-CN5NF could distinguish bacterial infection from sterile inflammation. In addition, [99mTc]Tc-CN5NF had higher abscess/blood and abscess/muscle ratios. SPECT image of [99mTc]Tc-CN5NF showed that there was a clear accumulation in the infection site, suggesting that it could be a potential bacterial infection imaging radiotracer.

Highlights

In the 18th and 19th centuries, public health has developed significantly
In many countries, the overuse of antibiotics has led to the appearance of drug-resistant bacteria, which greatly restrict the effect of the use of antibiotics
18 F-2-Fluoro-2-deoxy-D-glucose ([18 F]FDG) have already been used for infection imaging in clinics. It cannot distinguish between bacterial infection and sterile inflammation [10]

Summary

Introduction

In the 18th and 19th centuries, public health has developed significantly. By the 20th century, the treatment of infections had been greatly improved due to the discovery of antibiotics. Taking into account that patients with inflammation may develop different diseases at the same time, clinical testing may not always detect a clear cause of the inflammation, which will lead to delays in treatment and the abuse of antibiotics. Compared with CT and MRI, nuclear medicine technologies, such as positron emission tomography (PET) and single-photon emission computed tomography (SPECT), are based on metabolic changes due to physical, chemical, and biochemical alterations in organs These technologies can detect lesions at an early stage [6,7,8]. 18 F-2-Fluoro-2-deoxy-D-glucose ([18 F]FDG) have already been used for infection imaging in clinics It cannot distinguish between bacterial infection and sterile inflammation [10]. Radiolabeled 1-(20 -deoxy-20 -fluoro-βD-arabinofuranosyl)-5-iodouracil (FIAU) ([124 I]-FIAU) PET imaging cannot sensitively and detect bacterial infection in pulmonary or musculoskeletal systems [16]

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