title: 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.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, Sinhgad Institute of Pharmaceutical Sciences, Lonavala, Pune, India.
authors.forename: Nikhilesh
authors.initials: N
authors.lastname: Arya
authors.forename: Manoj K
authors.initials: MK
authors.lastname: Munde
authors.forename: Jaya
authors.initials: J
authors.lastname: Dwivedi
authors.forename: Archana Y
authors.initials: AY
authors.lastname: Jagdale
authors.forename: Kishor S
authors.initials: KS
authors.lastname: Jain
mesh_terms: D000818:Animals; D001384:Azetidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015415:Biomarkers / Q000097:blood; D002784:Cholesterol / Q000097:blood; D004195:Disease Models, Animal; D015195:Drug Design; D015248:Gemfibrozil / Q000494:pharmacology; D006949:Hyperlipidemias / Q000097:blood / Q000139:chemically induced / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007408:Intestinal Absorption / Q000187:drug effects; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D015394:Molecular Structure; D011092:Polyethylene Glycols; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood
chemical_list: C116379:2-azetidinone; D001384:Azetidines; D015415:Biomarkers; D000960:Hypolipidemic Agents; D011744:Pyrimidinones; D014280:Triglycerides; D011092:Polyethylene Glycols; D002784:Cholesterol; D015248:Gemfibrozil; C016811:tyloxapol
keywords: Antihyperlipidemic; Azetidinone; Gewald; Thienopyrimidines