title: Synthesis of fluorescent biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors.
abstract: 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).
authors.affiliation: Schering-Plough Research Institute, 2015 Galloping Hill Road MS 2800, Kenilworth, NJ 07033-0539, USA. duane.burnett@spcorp.com
authors.forename: Duane A
authors.initials: DA
authors.lastname: Burnett
authors.forename: Mary Ann
authors.initials: MA
authors.lastname: Caplen
authors.forename: Margaret E
authors.initials: ME
authors.lastname: Browne
authors.forename: Hongrong
authors.initials: H
authors.lastname: Zhau
authors.forename: Scott W
authors.initials: SW
authors.lastname: Altmann
authors.forename: Harry R
authors.initials: HR
authors.lastname: Davis
authors.forename: John W
authors.initials: JW
authors.lastname: Clader
mesh_terms: 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
chemical_list: C116379:2-azetidinone; D000924:Anticholesteremic Agents; D001384:Azetidines; D005456:Fluorescent Dyes; D010165:Palladium; D002784:Cholesterol; D000069438:Ezetimibe