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Excitation functions were measured by the activation method using the stacked-foil technique for the natMo(p,x)93(m+g),94m,g,95m,g,96(m+g),99mTc, 92m,95Nb reactions up to 18 MeV. The experimental results were compared with literature data and theoretical results from EMPIRE-3.2.2 code and TENDL. Special attention was paid to the 100Mo(p,2n)99mTc reaction which is very promising for the production of 99mTc at a cyclotron. In order to optimize the production conditions of some medically important Tc isotopes, the integral yields were estimated based on the measured cross sections.

Iodobenzamides are reported to possess some affinity for melanoma. This study describes the synthesis of a new benzamide analogue, N-(2-diethylamino-ethyl)-4-(4-chloro-nicotinamido)-5-[125I]iodo-2-methoxybenzamide ([125I]H4) designed to target melanoma. The synthesis was simply achieved in four steps. There were two PyCIU/DIPEA amide condensations and a transfer hydrogenation using an ammonium formate hydrogen donor. The radioiodination step was carried out with 125I via an electrophilic substitution reaction. The reaction conditions were optimized. The labeled compound was purified by HPLC. The maximum radiochemical yield was found to be 78% at a radiochemical purity of 98%. All compounds were characterized by MS and NMR techniques. The log P value for [125I]H4 was found as 3.96±0.5.

The broad-spectrum antibiotic agents have been demonstrated as promising diagnostic tools for early detection of infectious lesions. We set out ofloxacin (Oflo), a second-generation fluoroquinolone, 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 with ofloxacin. We found that radiolabeling in ethanol medium showed a 70% radiochemical yield of 125I-ofloxacin. The radioiodination was determined by means of TLC and HPLC. The cold labeled Oflo (127I-Oflo) 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. In conclusion, ofloxacine might be a promising target as an anti-inflammatory imaging agent.