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强效抗克氏锥虫药物CL 64855的致突变性

Mutagenicity of CL 64855, a potent anti-Trypanosoma cruzi drug.

作者信息

Ferreira R C, Ferreira L C

出版信息

Mutat Res. 1986 Jul;171(1):11-5. doi: 10.1016/0165-1218(86)90003-0.

DOI:10.1016/0165-1218(86)90003-0
PMID:3523230
Abstract

The nitroimidazole-thiadiazole derivative CL 64855 (2-amino-5 (1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole), a potent antimicrobial agent with curative action against Trypanosoma cruzi, was assayed in the Salmonella/microsome test. CL 64855 proved to be a potent mutagen to the frameshift indicator tester strains TA98 and TA102. No activity was observed with the base-pair substitution mutagen indicator strain TA100 in spot tests. No significant increase in the number of induced mutants could be detected in the presence of rat-liver microsome fraction. The excision-repair-deficient strain TA98 was much more sensitive to the killing action of CL 64855 than TA102, a repair-proficient strain. Possible differences among the mutagenic effects of CL 64855 and those observed with other anti-trypanosomal drugs are discussed.

摘要

硝基咪唑 - 噻二唑衍生物CL 64855(2 - 氨基 - 5(1 - 甲基 - 5 - 硝基 - 2 - 咪唑基)-1,3,4 - 噻二唑)是一种对克氏锥虫有治疗作用的强效抗菌剂,已在沙门氏菌/微粒体试验中进行了测定。结果证明,CL 64855对移码指示测试菌株TA98和TA102是一种强效诱变剂。在斑点试验中,碱基对替代诱变指示菌株TA100未观察到活性。在存在大鼠肝脏微粒体组分的情况下,未检测到诱导突变体数量的显著增加。切除修复缺陷型菌株TA98对CL 64855的杀伤作用比修复 proficient型菌株TA102敏感得多。文中讨论了CL 64855的诱变作用与其他抗锥虫药物所观察到的诱变作用之间可能存在的差异。

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