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以氨三乙酸和甲硝羟乙唑为原料合成了甲硝羟乙唑衍生物。经元素分析。mp测定,TLC,纸电泳,紫外及红外光谱扫描等一系列分析证明为甲硝羟乙唑衍生物(CM),其分子式为C_(18)H_(2(?))O_(10)N_7·1/2H_2O。经~(99m)Tc标记后,在荷S_(180)小鼠中有浓集于肿瘤的作用。静脉注射后24小时内,肿瘤中始终维持在较多的水平,肿瘤与脑和肌肉组织的放射性强度比值均分别在10及5左右,有肿瘤定位作用,在脑内含量低,降低了神经毒副作用。与钙鳌合后,对肉瘤180有辐射增敏作用,将另文报道。认为是一个颇有希望的新型肿瘤定位辐射增敏剂。
The metronidazole derivatives were synthesized from nitrilotriacetic acid and metronidazole. After elemental analysis. A series of analyzes such as mp, TLC, paper electrophoresis, UV and IR spectroscopy proved that the metronidazole derivative (CM) has the molecular formula C 18 H 2 O 2 O 10 N 7 · 1 / 2H_2O. After ~ (99m) Tc labeling, it has the function of concentrating tumor in S_ (180) mice. Intravenous injection within 24 hours, the tumor has always been maintained at more levels, tumors and brain and muscle radioactivity intensity ratio were 10 and 5, respectively, tumor localization, low in the brain, reducing the nerve toxicity side effect. Chelated with calcium, the radiation on the sarcoma 180 sensitization, will be reported in another article. It is considered as a promising new tumor targeting radiosensitizer.