الفهرس 
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Abstract
The broad-spectrum antibiotic agents have been demonstrated aspromising diagnostic tools for early detection of infectious lesions. We will study radioiodination process for fluoroquinolones.We set out Ofloxacin (Oflo) and Levofloxacin (levo), a second-generation fluoroquinolones, for the radioiodination process. In particular, this was carried out with 125I via an electrophilic substitution reaction. The radiochemical yield was influenced by different factors; drug concentration, different oxidizing agents, e.g. chloramine-T, iodogen and n-bromosuccinimide, pH of medium, reaction time, temperature and different organic media. These parameters were studied to optimize the best conditions for labeling ofloxacin and levofloxacin. For Ofloxacin we found that radiolabeling in ethanol medium showed a 69 % radiochemical yield of 125I-ofloxacin. The radioiodination was determined by means of TLC and HPLC. The cold labeled Oflo (127IOflo) was prepared and controlled by HPLC. The cold labeled Oflo was also confirmed by NMR and MS techniques. Furthermore, biodistribution studies for labeled 125I-Oflo were examined in two independent groups (3 mice in each one); control and E. Coli-injected (inflamed). The radiotracer showed a good localization in muscle of thigh for inflamed group as compared to control. For Levofloxacin we found that radiolabeling in ethanol medium showed a 74%.The radioiodination was determined by means of TLC and HPLC. The cold labeled Levo (127I-Levo) was prepared and controlled by HPLC. Furthermore, biodistribution studies for labeled 125I-Levo were examined in two independent groups (3 mice in each one); control and E. Coli-injected (inflamed). The radiotracer showed a localization in muscle of thigh for inflamed group but lower than that in biodistribution studies for labeled 125I-Oflo. In conclusion, ofloxacine and levofloxacin might be a promising target as an anti-inflammatory imaging agent.