Carboxy-substituted 2-azetidinones as cholesterol absorption inhibitors.
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 cholesterol absorption inhibition.
Vaccaro
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Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
Sher
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Davis
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D000818:Animals; D000924:Anticholesteremic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001384:Azetidines / Q000737:chemistry* / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood / Q000378:metabolism*; D006224:Cricetinae; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship
C116379:2-azetidinone; D000924:Anticholesteremic Agents; D001384:Azetidines; D002784:Cholesterol