Carboxy-substitutes 2-azetidinones as cholesterol absorption inhibitors

Article abstract of DOI:10.1016/S0960-894X(98)00009-2

Metabolism initiated SAR studies led to the discovery of a new class of potent 2-azetidinone cholesterol absorption inhibitors. These studies found that a heteroatom at the para position of the C-4 phenyl ring is not a requirement for cholesterol absorption inhibition as was suggested by earlier findings. Substitution of Ph-linker-COOR for PhOMe at the C-4 position enhanced absorption inhibition.