PMID: 9541655Apr 29, 1998Paper

Synthesis, metabolism and structure-mutagenicity relationships of novel 4-nitro-(imidazoles and pyrazoles) in Salmonella typhimurium

Mutation Research
P HreliaG Cantelli-Forti

Abstract

A new series of 4-nitro-(imidazoles and pyrazoles) were synthesized as novel antimycotics and tested for their activation to mutagenic forms using Salmonella typhimurium TA98 and TA100, in the presence and in the absence of metabolic activation. TA100NR, TA100/1,8-DNP6, YG1026 and YG1029 strains were employed to identify a specific metabolic reaction which governs the mutagenic potency. Derivatives in the pyrazole group were generally found to be non mutagenic and active imidazoles were weak-direct-acting mutagens. For most of the compounds the mutagenic responses in TA98 were absent or 12- to 22-fold lower compared to TA100. The presence of a methyl or a benzylic group on the imidazole ring and substituents on the N1 and N3 positions were determinant for mutagenicity. Metabolism by bacterial enzyme systems was important to the expression of genotoxicity. Active compounds showed no mutagenicity toward the strain defective in classical nitroreductase and increased mutagenicity, from 2- to 7-fold depending on the test compound, toward the corresponding overproducing bacteria. On the other hand, compounds displayed reduced mutagenicity to the O-acetyltransferase strain without having increased activity in the corresponding overpro...Continue Reading

References

Mar 1, 1975·Proceedings of the National Academy of Sciences of the United States of America·J McCannB N Ames
Aug 1, 1988·European Journal of Clinical Microbiology & Infectious Diseases : Official Publication of the European Society of Clinical Microbiology·T J Walsh, A Pizzo
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May 1, 1981·Mutation Research·C E Voogd
Oct 15, 1982·Biochemical and Biophysical Research Communications·E C McCoyH S Rosenkranz

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Citations

Dec 14, 2002·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·T OrsièreG Duménil
Oct 22, 2010·Environmental and Molecular Mutagenesis·Kerry L DearfieldKristine L Witt
Jul 14, 2005·European Journal of Drug Metabolism and Pharmacokinetics·S Güniz KüçükgüzelSevim Rollas

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