Mutagenicity of a series of 25 nitroimidazoles and two nitrothiazoles in Salmonella typhimurium.
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.
D009152:Mutagenicity Tests; D009153:Mutagens; D009154:Mutation; D009560:Niridazole / Q000494:pharmacology*; D009593:Nitroimidazoles / Q000494:pharmacology*; D012486:Salmonella typhimurium / Q000187:drug effects; D013045:Species Specificity; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology
D009153:Mutagens; D009593:Nitroimidazoles; D013844:Thiazoles; D009560:Niridazole