2011
DOI: 10.1039/c1mt00068c
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99mTc-labeling of ciprofloxacin and nitrofuryl thiosemicarbazone using fac-[99mTc(CO)3(H2O)3] core: evaluation of their efficacy as infection imaging agents

Abstract: The aim of this study was to radiolabel ciprofloxacin (Cip) and nitrofuryl thiosemicarbazone (NFT) with the fac-[(99m)Tc(CO)(3)(H(2)O)(3)](+) core and to evaluate the ability of the radiopharmaceuticals as tracers in detecting sites of infection. Cip and NFT were radiolabeled with the fac-[(99m)Tc(CO)(3)(H(2)O)(3)](+) core and characterized by RHPLC. The stabilities of the preparations were evaluated in saline and rat serum. In vitro binding studies of the radiopharmaceuticals with S. aureus were performed. Bi… Show more

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Cited by 21 publications
(12 citation statements)
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“…Multiple antibiotics with a variety of mechanisms of action such as ciproflaxicin (7,8) and nitrofuryl thiosemicarbazone (7), fluoroquinolone (9), isoniazid (10), ofloxacin (11,12), cephalosporin (13), clindamycin (14), doxycycline (15), ceftizoxime (16,17), cefotaxime (18), tinidazole (19), sulfadiazine (20), tazobactam (21) and metronidazole (22) were radiolabeled with 99m Tc to enable SPECT imaging in the pre-clinical models of infection. The majority of the authors employed Sn(+2) salts as the reducing agents for 99m Tc which produced [ 99m Tc-O](3+) core, while in several publications 99m Tc carbonyl or [ 99m Tc-N](2+) cores were utilized (7,8,11). The smaller size of 99m Tc carbonyl core might be less perturbing to the molecular structure of antibiotic molecules.…”
Section: Imaging Bacterial Infections With Radiolabeled Antibiotics S...mentioning
confidence: 99%
“…Multiple antibiotics with a variety of mechanisms of action such as ciproflaxicin (7,8) and nitrofuryl thiosemicarbazone (7), fluoroquinolone (9), isoniazid (10), ofloxacin (11,12), cephalosporin (13), clindamycin (14), doxycycline (15), ceftizoxime (16,17), cefotaxime (18), tinidazole (19), sulfadiazine (20), tazobactam (21) and metronidazole (22) were radiolabeled with 99m Tc to enable SPECT imaging in the pre-clinical models of infection. The majority of the authors employed Sn(+2) salts as the reducing agents for 99m Tc which produced [ 99m Tc-O](3+) core, while in several publications 99m Tc carbonyl or [ 99m Tc-N](2+) cores were utilized (7,8,11). The smaller size of 99m Tc carbonyl core might be less perturbing to the molecular structure of antibiotic molecules.…”
Section: Imaging Bacterial Infections With Radiolabeled Antibiotics S...mentioning
confidence: 99%
“…The fac-[ 99m TcIJCO) 3 IJH 2 O) 3 ] + precursor was prepared as per the reported method. 28,29 Briefly, an aqueous solution (1.5 mL) containing Na/K tartrate (15 mg), Na 2 CO 3 (4 mg) and NaBH 4 (5.5 mg) was purged with carbon monoxide for 6-8 min at room temperature, followed by the addition freshly extracted aqueous 99m TcO 4 − (0.5 mL, 185-370 MBq), and the mixture was heated at 80°C for 20 min. The pH was adjusted between 6.5 and 7 with a mixture of 0.5 M phosphate buffer (pH 7.5) : 1 N HCl (1 : 3) and the purity of the tricarbonyl precursor was analysed by HPLC.…”
Section: Radiolabelingmentioning
confidence: 99%
“…They have a bactericidal effect and are therefore used to treat bacterial infections. The structure of quinolones allows various modifications to the molecule to be introduced without it losing its properties and therapeutic effect [13], so they are applied in radiopharmaceuticals for imaging bacterial infections after labelling with 99m Tc [11,[14][15][16][17][18] or 18 F [10,19,20].…”
Section: Introductionmentioning
confidence: 99%