Relative hepatotoxicity of 2-(substituted phenyl)thiazoles and substituted thiobenzamides in mice: evidence for the involvement of thiobenzamides as ring cleavage metabolites in the hepatotoxicity of 2-phenylthiazoles

Toxicol Lett. 1996 May;85(2):101-5. doi: 10.1016/0378-4274(96)03646-6.

Abstract

The hepatotoxicity of the 3 isomers of para-substituted thiobenzamides and the 3 isomers of 2-(para-substituted phenyl)-4-methylthiazoles was evaluated in mice depleted of glutathione (GSH) by pretreatment with buthionine sulfoximine (BSO). In accordance with previous studies with the rat, p-methoxythiobenzamide was more toxic than thiobenzamide, and conversely p-chlorothiobenzamide was markedly less toxic as assessed by serum alanine aminotransferase (ALT) activity. The hepatotoxicity of 2-phenyl-4-methylthiazole was also altered by the addition of para-substituents to the phenyl ring in the same way as observed for thiobenzamide derivatives: the rank order of toxicity was 4-methylthiazoles having p-methoxyphenyl > phenyl >> p-chlorophenyl at the 2-position. This good correlation of the rank order of hepatotoxicity between series of 2-(para-substituted phenyl)-4-methylthiazoles and para-substituted thiobenzamides supports the concept that thiobenzamides as ring cleavage metabolites play a role in the hepatotoxicity of 2-phenylthiazole derivatives.

MeSH terms

  • Alanine Transaminase / blood
  • Animals
  • Glutathione / metabolism
  • Liver / drug effects*
  • Male
  • Methionine Sulfoximine / pharmacology
  • Mice
  • Mice, Inbred ICR
  • Pyruvaldehyde / urine
  • Structure-Activity Relationship
  • Thiazoles / chemistry
  • Thiazoles / toxicity*
  • Thioamides / chemistry
  • Thioamides / metabolism
  • Thioamides / toxicity*

Substances

  • Thiazoles
  • Thioamides
  • Methionine Sulfoximine
  • Pyruvaldehyde
  • thiobenzamide
  • Alanine Transaminase
  • Glutathione