Cantelli-Forti G, Aicardi G, Guerra M C, Barbaro A M, Biagi G L
Teratog Carcinog Mutagen. 1983;3(1):51-63. doi: 10.1002/1520-6866(1990)3:1<51::aid-tcm1770030107>3.0.co;2-l.
Twenty-five 5-nitroimidazole and two 5-nitrothiazole derivatives were tested for mutagenicity as well as for antibacterial activity in Salmonella typhimurium TA-100 strain. Many of these compounds such as metronidazole, azanidazole, nimorazole, carnidazole, ornidazole, tinidazole, etc are extensively used in human chemotherapy, and some of them were recently synthetized for possible clinical trials as hypoxic cell specific radiosensitizers. Both mutagenic and antibacterial activity were shown for 22 of the test compounds. The high correlation between mutagenic and antibacterial activity supports the hypothesis of a same mechanism for both activities. The present results confirm that the mutagenicity of the nitroheterocyclic compounds is not separated from other biological activities, such as antimicrobial activity.
对25种5-硝基咪唑和2种5-硝基噻唑衍生物进行了鼠伤寒沙门氏菌TA-100菌株的致突变性和抗菌活性测试。这些化合物中的许多,如甲硝唑、阿扎硝唑、尼莫唑、卡硝唑、奥硝唑、替硝唑等,在人类化疗中被广泛使用,其中一些最近被合成用于可能的临床试验,作为缺氧细胞特异性放射增敏剂。22种测试化合物均显示有致突变性和抗菌活性。致突变性和抗菌活性之间的高度相关性支持了这两种活性具有相同机制的假设。目前的结果证实,硝基杂环化合物的致突变性与其他生物活性,如抗菌活性,并非相互独立。