Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
Fluorescent analogues of the cholesterol absorption inhibitor (CAI), Sch 58235, have been designed and synthesized as single enantiomers. Biological testing reveals that they are potent CAIs and are suitable tools for the investigation of the azetidinone CAI mechanism of action (MOA).
Burnett
Duane A
DA
Schering-Plough Research Institute, 2015 Galloping Hill Road MS 2800, Kenilworth, NJ 07033-0539, USA. duane.burnett@spcorp.com
Caplen
Mary Ann
MA
Browne
Margaret E
ME
Zhau
Hongrong
H
Altmann
Scott W
SW
Davis
Harry R
HR
Clader
John W
JW
D000818:Animals; D000924:Anticholesteremic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001384:Azetidines / Q000737:chemistry* / Q000494:pharmacology; D002384:Catalysis; D002784:Cholesterol / Q000493:pharmacokinetics*; D015195:Drug Design; D000069438:Ezetimibe; D005456:Fluorescent Dyes / Q000138:chemical synthesis*; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D010165:Palladium; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
C116379:2-azetidinone; D000924:Anticholesteremic Agents; D001384:Azetidines; D005456:Fluorescent Dyes; D010165:Palladium; D002784:Cholesterol; D000069438:Ezetimibe