Synthesis and quantitative structure-activity relationships of antihyperlipaemic 2-substituted thieno[3,2-d]pyrimidin-4(3H)-ones

Arzneimittelforschung. 1996 Mar;46(3):273-6.

Abstract

The synthesis, antihyperlipaemic evaluation and quantitative structure-activity relationships (QSAR) of two series of thieno[3,2-d]pyrimidin-4-one derivatives are reported. While most of the compounds in these series were found to exhibit antihyperlipaemic activity, the QSAR study of these two series indicated a positive influence of only the electronic nature of the 2-substitutents on the biological activity. The lipophilic and the steric parameters did not appear to be significant.

MeSH terms

  • Animals
  • Chemical Phenomena
  • Chemistry, Physical
  • Cholesterol / blood
  • Chromatography, High Pressure Liquid
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / pharmacology*
  • Indicators and Reagents
  • Molecular Conformation
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Rats
  • Rats, Wistar
  • Regression Analysis
  • Spectrophotometry, Infrared
  • Structure-Activity Relationship

Substances

  • Hypolipidemic Agents
  • Indicators and Reagents
  • Pyrimidines
  • Cholesterol