Design, synthesis, and antihyperlipidemic evaluation of novel 2-[1-(substitutedphenyl)-4-oxo-azetidin-2-yl]-5,6-disubstitutedthieno[2,3-d]pyrimidin-4(3H)-ones

Arch Pharm (Weinheim). 2013 Aug;346(8):588-95. doi: 10.1002/ardp.201300001. Epub 2013 Jul 24.

Abstract

Novel thienopyrimidine derivatives of azetidinone possessing the combined features of the cholesterol absorption inhibitor drug ezetimibe and potential antihyperlipidemic 2-substitutedthienopyrimidin-4-ones were synthesized and characterized by spectroscopic data and elemental analysis. These compounds were evaluated for their lipid-lowering activity in Wistar albino rats. Some of them showed significant lipid-lowering effects comparable to those of the standard drug, gemfibrozil, at the same dose levels.

Keywords: Antihyperlipidemic; Azetidinone; Gewald; Thienopyrimidines.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Azetidines / chemical synthesis*
  • Azetidines / pharmacology*
  • Biomarkers / blood
  • Cholesterol / blood
  • Disease Models, Animal
  • Drug Design*
  • Gemfibrozil / pharmacology
  • Hyperlipidemias / blood
  • Hyperlipidemias / chemically induced
  • Hyperlipidemias / drug therapy*
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / pharmacology*
  • Intestinal Absorption / drug effects
  • Intestinal Mucosa / metabolism
  • Intestines / drug effects
  • Molecular Structure
  • Polyethylene Glycols
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology*
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Triglycerides / blood

Substances

  • 2-azetidinone
  • Azetidines
  • Biomarkers
  • Hypolipidemic Agents
  • Pyrimidinones
  • Triglycerides
  • Polyethylene Glycols
  • Cholesterol
  • Gemfibrozil
  • tyloxapol