2-Azetidinone derivatives: Design, synthesis and evaluation of cholesterol absorption inhibitors

Fourteen new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, and three of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in rats, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum. (c) 2008 Elsevier Masson SAS. All rights reserved.