2-Azetidinone cholesterol absorption inhibitors: increased potency by substitution of the C-4 phenyl ring.
SAR studies directed towards the optimization of 2-azetidinone cholesterol absorption inhibitors led to the discovery of 11a, the most potent cholesterol absorption inhibitor yet identified.
Vaccaro
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WD
Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.
Sher
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R
Davis
H R
HR
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; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013329:Structure-Activity Relationship
C116379:2-azetidinone; D000924:Anticholesteremic Agents; D001384:Azetidines; D002784:Cholesterol