Novel pyrimidine and 1,3,5-triazine hypolipidemic agents

J Med Chem. 1984 Dec;27(12):1621-9. doi: 10.1021/jm00378a016.

Abstract

New compounds were synthesized by changing the substituents of a trisubstituted pyrimidine, i.e., [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio] acetic acid, a potent hypolipidemic agent, impaired, however, by a marked hepatomegaly-inducing effect. The structural variations led to the subsidence (14b, i.e., 4-chloro-2-(dimethylamino)-6-[(2,3-dimethylphenyl)amino]pyrimidine) or to the reduction (18b, [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]amino] acetic acid) of said untoward effect but still maintained the hypolipidemic effect that, although markedly decreased, still proves significant for serum cholesterol and triglycerides (18b) or for serum triglycerides only (14b).

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Chemical Phenomena
  • Chemistry
  • Cholesterol / blood
  • Drug Evaluation, Preclinical
  • Hypolipidemic Agents / chemical synthesis*
  • Indicators and Reagents
  • Lipoproteins / blood
  • Liver / anatomy & histology
  • Liver / drug effects
  • Magnetic Resonance Spectroscopy
  • Male
  • Mass Spectrometry
  • Organ Size / drug effects
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Structure-Activity Relationship
  • Triglycerides / blood

Substances

  • Hypolipidemic Agents
  • Indicators and Reagents
  • Lipoproteins
  • Pyrimidines
  • Triglycerides
  • Cholesterol