title: Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity.
abstract: A number of newly synthesized 2-[4-(hetero)aromatic]phenyl-2-hydroxy-tetrahydro-1,4-oxazine derivatives were found to inhibit lipid peroxidation (IC50 of the most potent was 20 microM) as well as rat squalene synthase (IC50 for most between 1-10 microM). Antidyslipidemic action was demonstrated in vivo: the most active compound decreased triglycerides, total cholesterol, and LDL-cholesterol of hyperlipidemic rats by 64, 67, and 82%, respectively, at 56 micromol/kg (ip). Most of the novel compounds are more active than the structurally related and reference biphenyl-morpholine, pointing to useful structural approaches for the design of antiatherosclerotic agents.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, University of Athens, 15771 Athens, Greece. angeliki@pharm.uoa.gr
authors.forename: Angeliki P
authors.initials: AP
authors.lastname: Kourounakis
authors.forename: Christos
authors.initials: C
authors.lastname: Charitos
authors.forename: Eleni A
authors.initials: EA
authors.lastname: Rekka
authors.forename: Panos N
authors.initials: PN
authors.lastname: Kourounakis