Unambiguous synthesis of asymmetrically substituted chlorinated benzidines, and a study of their mutagenicity in the Ames test: potent activity of 3,5,3'-trichlorobenzidine

Mutagenesis. 1987 May;2(3):225-8. doi: 10.1093/mutage/2.3.225.

Abstract

3,5-Dichlorobenzidine and 3,5,3'-trichlorobenzidine were prepared by the reaction of 2,6-dichloronitrosobenzene with aniline and 2-chloroaniline, respectively, to give the appropriate substituted azobenzene; reduction and rearrangement gave the desired benzidine derivatives. The products were purified and characterized by mass spectrometry and [1H] nuclear magnetic resonance spectroscopy. The mutagenic activities of the chlorinated benzidines were determined, using the Ames tester strain TA98. 3,5,3'-Trichlorobenzidine is the most potent benzidine derivative yet reported. The activities of five chlorinated benzidines are compared, and rules for the effect of substitution on activity are discussed.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzidines / chemical synthesis*
  • Benzidines / pharmacology
  • Biotransformation
  • Chlorides
  • Cricetinae
  • Indicators and Reagents
  • Mass Spectrometry
  • Microsomes, Liver / metabolism
  • Mutagenicity Tests
  • Mutagens / chemical synthesis*
  • Mutation*
  • Salmonella typhimurium / drug effects

Substances

  • Benzidines
  • Chlorides
  • Indicators and Reagents
  • Mutagens