Synthesis and evaluation of 99mTc-moxifloxacin, a potential infection specific imaging agent

Chattopadhyay, Sankha; Das, Sujata Saha; Chandra, Sarmila; Kyle, Dennis E.; Mishra, Mridula; Sarkar, B. R.; Sinha, Samarendu; Ganguly, Shantanu

doi:10.1016/j.apradiso.2009.10.030

Cited by 63 publications

(11 citation statements)

References 6 publications

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“…Experimental data of the liver and kidney uptakes of 21 Tc99m labeled quinolone antibiotics were taken from the recently published papers [14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30]. The biodistribution data collected was reported in rats and mice and experimentally induced infection using Staphylococcus aureus or E. coli, after two hours of bacterial induction.…”

Section: Methodsmentioning

confidence: 99%

Quantitative structure–activity relationship analysis to elucidate the clearance mechanisms of Tc-99m labeled quinolone antibiotics

Salahinejad¹,

Mirshojaei²

2015

J Radioanal Nucl Chem

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This study aims to establish molecular modeling methods for predicting the liver and kidney uptakes of Tc-99m labeled quinolone antibiotics. Some three-dimensional quantitative-activity relationships (3D-QSAR) models were developed using comparative molecular field analysis and grid-independent descriptors procedures. As a first report on 3D-QSAR modeling, the predicted liver and kidney uptakes for quinolone antibiotics were in good agreement with the experimental values. The obtained results confirm the importance of hydrophobic interactions, size and steric hindrance of antibiotic molecules in their liver uptakes, while the electrostatic interactions and hydrogen bonding ability have impressive effects on their kidney uptakes.

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Section: Methodsmentioning

confidence: 99%

Quantitative structure–activity relationship analysis to elucidate the clearance mechanisms of Tc-99m labeled quinolone antibiotics

Salahinejad¹,

Mirshojaei²

2015

J Radioanal Nucl Chem

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“…It was studied in rats and rabbits after the induction of a septic inflammation with E. coli in the thigh muscle. On images it was possible to notice the infected site in a clear way, with a specific accumulation six times higher than in normal tissues [76]. …”

Section: Fluoroquinolonesmentioning

confidence: 99%

Imaging bacteria with radiolabelled quinolones, cephalosporins and siderophores for imaging infection: a systematic review

Auletta

Galli

Lauri

et al. 2016

Clin Transl Imaging

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Bacterial infections are still one of the main causes of patient morbidity and mortality worldwide. Nowadays, many imaging techniques, like computed tomography or magnetic resonance imaging, are used to identify inflammatory processes, but, although they recognize anatomical modifications, they cannot easily distinguish bacterial infective foci from non bacterial infections. In nuclear medicine, many efforts have been made to develop specific radiopharmaceuticals to discriminate infection from sterile inflammation. Several compounds (antimicrobial peptides, leukocytes, cytokines, antibiotics…) have been radiolabelled and tested in vitro and in vivo, but none proved to be highly specific for bacteria. Indeed factors, including the number and strain of bacteria, the infection site, and the host condition may affect the specificity of tested radiopharmaceuticals. Ciprofloxacin has been proposed and intensively studied because of its easy radiolabelling method, broad spectrum, and low cost, but at the same time it presents some problems such as low stability or the risk of antibiotic resistance. Therefore, in the present review studies with ciprofloxacin and other radiolabelled antibiotics as possible substitutes of ciprofloxacin are reported. Among them we can distinguish different classes, such as cephalosporins, fluoroquinolones, inhibitors of nucleic acid synthesis, inhibitors of bacterial cell wall synthesis and inhibitors of protein synthesis; then also others, like siderophores or maltodextrin-based probes, have been discussed as bacterial infection imaging agents. A systematic analysis was performed to report the main characteristics and differences of each antibiotic to provide an overview about the state of the art of imaging infection with radiolabelled antibiotics.

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“…The promising results of the available infection radiotracers, together with our recently reported work [3][4][5][6][7][8][9][10][11][12][13][14][15], have motivated us to develop more sensitive and specific radiopharmaceuticals. Fleroxacin [FXN, 6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid] has recently been established as a novel trifluorinated quinolone antibiotic with promising broad spectrum activity against Gram-positive and Gram-negative bacteria.…”

Section: Introductionmentioning

confidence: 97%

Radiosynthesis and characterization of the 99mTc-fleroxacin complex: a novel Escherichia coli infection imaging agent

Shah

Khan

2011

Transition Met Chem

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Radiocomplexation of fleroxacin (FXN) with technetium-99m and its characterization in terms of in vitro stability in saline and serum solutions, in vitro binding with live and heat-killed Escherichia coli, and biodistribution in male Wistar rats (MWR) artificially infected with live and heat-killed E. coli was studied. The 99m Tc-FXN complex showed a radiochemical purity (RCP) yield of 98.10 ± 0.24% at 30 min using 125 lg of stannous fluoride, 74 MBq of sodium pertechnetate, and 2 mg of FXN. The complex was found to be more than 90% stable up to 4 h after constitution in normal saline. In serum, the emergence of 16.50% undesirable species was observed within 16 h of incubation at 37°C. The 99m Tc-FXN complex showed saturated in vitro binding with E. coli with a maximum value of 65.00% at 90 min. A fivefold increase in uptake of the complex was noted in the infected when compared with the inflamed and normal muscle of the MWR infected with live E. coli. The stable radiochemical profile in saline and serum, saturated in vitro binding with E. coli and increased uptake in the infected muscle, confirmed the potential of the 99m Tc-FXN complex as an E. coli infection imaging agent.

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Synthesis and evaluation of 99mTc-moxifloxacin, a potential infection specific imaging agent

Cited by 63 publications

References 6 publications

Quantitative structure–activity relationship analysis to elucidate the clearance mechanisms of Tc-99m labeled quinolone antibiotics

Quantitative structure–activity relationship analysis to elucidate the clearance mechanisms of Tc-99m labeled quinolone antibiotics

Imaging bacteria with radiolabelled quinolones, cephalosporins and siderophores for imaging infection: a systematic review

Radiosynthesis and characterization of the 99mTc-fleroxacin complex: a novel Escherichia coli infection imaging agent

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