Radiosynthesis of 99mTc(CO)3-Clinafloxacin Dithiocarbamate and Its Biological Evaluation as a Potential Staphylococcus aureus Infection Radiotracer

Shah, Syed Qaiser; Khan, Muhammad Rafiullah; Ali, Sadiq

doi:10.1007/s13139-011-0106-8

Cited by 23 publications

(6 citation statements)

References 16 publications

(21 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Shah et al studied three additional radiolabelled antibiotics (Scheme 1) derived from last resort fluoroquinolones [38]: 99m Tc-labelled garenoxacin dithiocarbamate [39], 99m Tc-clinafloxacin dithiocarbamate [40], and 99m TcN-gatifloxacin dithiocarbamate [41]. In biodistribution studies in rats all these radiolabelled antibiotics demonstrated good uptake in multi-resistant S. aureus and penicillin-resistant streptococcal infections (abscess-to-muscle ratios between 4.4 and 6.5).…”

Section: Bacterial Infection Imaging Agents Based On Antibioticsmentioning

confidence: 99%

An update on radiotracer development for molecular imaging of bacterial infections

Welling

Hensbergen

Bunschoten

et al. 2019

Clin Transl Imaging

View full text Add to dashboard Cite

Background Bacterial infections are still a major global healthcare problem. To combat the increasing antimicrobial resistance, early diagnosis of bacterial infections-including the identification of bacterial species-is needed to improve antibiotic stewardship and to help reduce the use of broad-spectrum antibiotics. To aid successful targeted antibiotic treatment, specific detection and localisation of infectious organisms is warranted. Nuclear medicine imaging approaches have been successfully used to diagnose bacterial infections and to differentiate between pathogen induced infections and sterile inflammatory processes. Aim In this comprehensive review we present an overview of recent developments in radiolabelled bacterial imaging tracers. Methods The PubMed/MEDLINE and Embase (OvidSP) literature databases were systematically searched for publications on SPECT and PET on specific imaging of bacterial using specific guidelines with MeSH-terms, truncations, and completion using cross-references. Tracers in literature that was extensively reviewed before 2016 were not included in this update. Where possible, the chemical structure of the radiolabelled compounds and clinical images were shown. Results In 219 original articles pre-clinical and clinical imaging of bacterial infection with new tracers were included. In our view, the highest translational potential lies with tracers that are specific to target the pathogens: e.g., 99m Tc-and 68 Galabelled UBI 29-41 , 99m Tc-vancomycin, m-[ 18 F]-fluoro-PABA, [methyl-11 C]-D-methionine, [ 18 F]-FDS, [ 18 F]-maltohexaose and [ 18 F]-maltotriose. An encouraging note is that some of these tracers have already been successfully evaluated in clinical settings. Conclusion This review summarises updates in tracer development for specific (pre-clinical and clinical) imaging of bacterial infections. We propsed some promising tracers that are likely to become innovative standards in the clinical setting in the near feature.

show abstract

Section: Bacterial Infection Imaging Agents Based On Antibioticsmentioning

confidence: 99%

An update on radiotracer development for molecular imaging of bacterial infections

Welling

Hensbergen

Bunschoten

et al. 2019

Clin Transl Imaging

View full text Add to dashboard Cite

show abstract

“…A wide variety of radiolabeled agents have been evaluated for their potential to distinguish between microbial infectious lesions (Auletta et al., 2016; Salmanoglu et al., 2018). Fluoroquinolones, some cephalosporins, and most other antibacterial agents have been radiolabeled for bacterial infection imaging with promising results (Shah et al., 2011; Yurt Lambrecht et al., 2008). Also, several β ‐lactam antibiotics have been labeled with 99m Tc, including cefazolin, ceftizoxime, ceftriaxone, amoxicillin (Fazli et al., 2013; Mostofa et al., 2010; Shahzadi et al., 2015).…”

Section: Resultsmentioning

confidence: 99%

In vitro evaluation of ^99mTc‐sultamicillin for infection imaging

Durkan

Tunçel

Yurt

2021

Biopharm & Drug Disp

View full text Add to dashboard Cite

Early detection of the site of infection non‐invasively with radiolabeled molecules is important for the success of treatment. Technetium‐99m labeled antibiotics have the potential to discriminate between bacterial infection and sterile inflammation. Sultamicillin is the tosylate salt of the double ester of sulbactam plus ampicillin. In this study, sultamicillin was labeled with 99mTc according to the stannous chloride method. Quality control studies of radiolabeled sultamicillin were performed by radiochromatographic methods. In vitro binding assays were performed in live and heat‐killed gram‐positive Staphylococcus aureus and gram‐negative Escherichia coli strains. The radiolabeling yield of 99mTc‐sultamicillin was determined as 97.8% ± 3.1% (n = 5). The maximum bacterial uptake of 99mTc‐sultamicillin was 80.7% ± 11.00% at 4 h for living S. aureus and 93.2% ± 4.40% at 2 h for E. coli. Bacterial uptake study results show that sultamicillin has the potential to be a nuclear imaging agent, especially in infections caused by gram‐negative E. coli and gram‐positive S. aureus.

show abstract

“…HMNPs-C n were used for 99 Tc m labeling in order to study the effect of these encapsulation capabilities on the 99 Tc m . The radiolabeling of HMNPs-C n was carried out using the reported method [23]. Brie y, 4.9 mCi of 100 µL sodium pertechnetate (Na 99 Tc m O 4 ) was mixed with 2 mL medical saline and 400 µl stannous chloride (SnCl 2 ) in a vial, which could reduce 99 Tc m (VII) into 99 Tc m (III) ions.…”

Section: Preparation Of Technetium-99m ( 99 Tc M ) Labeled Hollow Mag...mentioning

confidence: 99%

Fabricated HMNPs with Size Approaching ~100 nm for MMC Loading and Sustained-release, as well as Labeling 99Tcm

Yang

Chang

Dong

et al. 2022

Preprint

View full text Add to dashboard Cite

Herein, we developed the dual-function template method to fabricate hollow magnetic nano-spheres (denoted as HMNPs-Cn, n = 16, 18) with a mesoporous shell and hollow interior structure using alkyl chain trimethoxysilane templating. The microstructure of the HMNPs-Cn was investigated by means of XRD, FT-IR, EDS, SEM, TEM and N2-BET analyses. The shorter chain template directed formation of HMNPs-C16 with size of 119 nm, having disordered inkbottle type mesopores and saturation magnetization of 50.01 emu/g. It can be observed that, mitomycin C (MMC) loaded HMNPs-Cn hollow spheres showed a clear pH-dependent drug release behavior, having a higher release rate in acidic environments of pH 5.7. For the pH 5.7 and 7.4 release, the diffusion through HMNPs-Cn hollow spheres is the rate limiting step, the release kinetic for HMNPs-C16-MMC composites follows pseudo-first-order attributable to its special pore structure. For this reason the inner cavity of HMNPs-C16 could be labeled with radioisotope 99Tcm to study the magnetic targeting distribution of HMNPs-C16 in vivo, and its cytotoxicity against in vitro HeLa cells was also studied. These results indicate the potential of HMNPs-C16 in the magnetic targeted drug delivery system.

show abstract

Radiosynthesis of 99mTc(CO)3-Clinafloxacin Dithiocarbamate and Its Biological Evaluation as a Potential Staphylococcus aureus Infection Radiotracer

Abstract: Background Clinafloxacin dithiocarbamate (CNND) was radiolabeled with technetium-99m ( 99m

Cited by 23 publications

References 16 publications

An update on radiotracer development for molecular imaging of bacterial infections

An update on radiotracer development for molecular imaging of bacterial infections

In vitro evaluation of ^99mTc‐sultamicillin for infection imaging

Fabricated HMNPs with Size Approaching ~100 nm for MMC Loading and Sustained-release, as well as Labeling 99Tcm

Contact Info

Product

Resources

About

Radiosynthesis of 99mTc(CO)3-Clinafloxacin Dithiocarbamate and Its Biological Evaluation as a Potential Staphylococcus aureus Infection Radiotracer

Abstract: Background Clinafloxacin dithiocarbamate (CNND) was radiolabeled with technetium-99m ( 99m

Cited by 23 publications

References 16 publications

An update on radiotracer development for molecular imaging of bacterial infections

An update on radiotracer development for molecular imaging of bacterial infections

In vitro evaluation of 99mTc‐sultamicillin for infection imaging

Fabricated HMNPs with Size Approaching ~100 nm for MMC Loading and Sustained-release, as well as Labeling 99Tcm

Contact Info

Product

Resources

About

In vitro evaluation of ^99mTc‐sultamicillin for infection imaging