Synthesis, biodistribution and evaluation of 99mTc-sitafloxacin kit: a novel infection imaging agent

Qaiser, S.; Khan, Aakif Ullah; Khan, Muhammad Rafiullah

doi:10.1007/s10967-010-0470-3

Cited by 52 publications

(18 citation statements)

References 14 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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“…The radiochemical yield of the 99m Tc-TIN complex was determined using modified RP-HPLC (Shimadzu SCL-10 AVP system, with SDP-10 AVP UV detector operating at 254 nm, Packard 500 TR series flow scintillation analyzer, binary pump, using online degasser) method as reported, 14 briefly. Five microlitres of the 99m Tc-TIN complex was injected into the RP C-18 column (4.6 Â 150 mm, 5 mM) with a flow rate of 1 ml/min was employed for 20 min using a mobile phase of water:-acetonitrile (W:A)(10:90).…”

Section: Radiochemical Yield and Stability In Salinementioning

confidence: 99%

“…1,2 Nuclear medicine is offering a unique way of looking into infective process. The labelled antibiotics such as ciprofloxacin, [3][4][5] ciprofloxacin dithocarbamate, 6 cefoperazone, 7 lomefloxacin, ofloxacin, 8 cefuroxine, 9 pefloxacin, 10 kanamycin, 11 sparafloxacin, 12 moxifloxacin 13 and sitafloxacin 14 have shown promising results regarding specific infections but the resistant microorganism sucha s methicillin-resistant Staphylococcus aureus (MRSA) still poses a threat because of its resistant to a large number of antibiotics.…”

Section: Introductionmentioning

confidence: 99%

Radiosynthesis, biodistribution and scintigraphy of the ^99mTc‐Teicoplanin complex in artificially infected animal models

Shah¹,

Khan²,

Khan³

2010

Labelled Comp Radiopharmac

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Radiocomplexation of Teicoplanin (TIN), a new glycopeptide antibiotic with technetium-99m, was investigated. The 99m Tc-TIN complex was assessed for its radiochemical permanence, in vitro stability in serum, binding with methicillin-resistant Staphylococcus aureus (MRSA), biodistribution in Model Rats (MRT) and for scintigraphic precision in Model Rabbit (MRB). Radiochemically, a stable 99m Tc-TIN was observed with 98.9070.50% yield and remained staunch more than 90% up to 120 min, by mixing TIN, 1.5 mg in 0.5 ml of saline with 2.5 mCi sodium pertechnetate and 150 ml of stannous chloride dihydrate at pH 5.4. The 99m Tc-TIN was found stable in serum with an insignificant undesirable yield of free and unhydrolyzed technetium (5.2570.10 and 13.570.14%, n = 10) up to 120 min of incubation. The 99m Tc-TIN showed in vitro binding with MRSA in the range of 55-65%. The 99m Tc-TIN showed almost six-fold elevated uptake in the infected (IFT) muscle of the MRT as compared with the inflamed (IFM) and normal (NL) muscles. This higher uptake of the 99m Tc-TIN in the IFT was scintigraphically confirmed after the whole body scanning of the MRB. The radiochemical eternalness with high yield, in vitro stability in serum, binding with MRSA, significant biodistribution performance, and scintigraphic precision posed the 99m Tc-TIN, a new glycopeptide radiotracer for the infection imaging.

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“…The in-vitro and in-vivo results of our recently developed kits encouraged us to seek for more stable and specific infection imaging agents [3][4][5][6][7][8][9][10][11][12][13][14][15].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of the 99mtcn-Gemifloxacin Dithiocarbamate Complex: A Novel Streptococcus Pneumoniae Infection Imaging Agent

Khan¹

2013

J Mol Imag Dynamic

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Synthesis and biological evaluation of the 99m TcN-Gemifloxacin dithiocarbamate ( 99m TcN-GIND) complex was investigated in terms of radiochemical stability (RCP) in saline, serum, in-vitro binding with Streptococcus pneumoniae (S. pneumoniae) and biodistribution in male Wistar rats artificially infected with living and heat killed S. pneumoniae. The maximum RCP was 98.25 ± 0.30% at 30 min and decreased to 91.25 ± 0.34% within 240 min. The complex showed stable behavior (in-vitro) in serum at 37°C with a 14.35% undesirable side products within 16 h. The complex showed 71.25% in-vitro binding S. pneumoniae. The uptake of the complex in the infected muscle was six times higher than the inflamed and normal muscles of the MWR infected with living S. pneumoniae. The promising (in-vitro and in-vivo) radiochemical and biological behavior posed the 99m TcN-GIND complex as a potential radiotracer for S. pneumoniae infection.

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Synthesis, biodistribution and evaluation of 99mTc-sitafloxacin kit: a novel infection imaging agent

Cited by 52 publications

References 14 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

Radiosynthesis, biodistribution and scintigraphy of the ^99mTc‐Teicoplanin complex in artificially infected animal models

Synthesis and Biological Evaluation of the 99mtcn-Gemifloxacin Dithiocarbamate Complex: A Novel Streptococcus Pneumoniae Infection Imaging Agent

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Synthesis, biodistribution and evaluation of 99mTc-sitafloxacin kit: a novel infection imaging agent

Cited by 52 publications

References 14 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

Radiosynthesis, biodistribution and scintigraphy of the 99mTc‐Teicoplanin complex in artificially infected animal models

Synthesis and Biological Evaluation of the 99mtcn-Gemifloxacin Dithiocarbamate Complex: A Novel Streptococcus Pneumoniae Infection Imaging Agent

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Radiosynthesis, biodistribution and scintigraphy of the ^99mTc‐Teicoplanin complex in artificially infected animal models