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.

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.