title: Inhibitors of acyl CoA:cholesterol acyltransferase.
abstract: Conformational restriction of previously disclosed acyclic (diphenylethyl)diphenylacetamides led to the discovery of several potent inhibitors of acyl CoA:cholesterol acyltransferase (ACAT). cis-[2-(4-Hydroxyphenyl)-1-indanyl]diphenylacetamide (4a) was the most potent ACAT inhibitor identified (IC50 = 0.04 microM in an in vitro rat hepatic microsomal ACAT assay, ED50 = 0.72 mg/kg/day in cholesterol-fed hamster.
authors.affiliation: Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
authors.forename: W
authors.initials: W
authors.lastname: Vaccaro
authors.forename: C
authors.initials: C
authors.lastname: Amore
authors.forename: J
authors.initials: J
authors.lastname: Berger
authors.forename: R
authors.initials: R
authors.lastname: Burrier
authors.forename: J
authors.initials: J
authors.lastname: Clader
authors.forename: H
authors.initials: H
authors.lastname: Davis
authors.forename: M
authors.initials: M
authors.lastname: Domalski
authors.forename: T
authors.initials: T
authors.lastname: Fevig
authors.forename: B
authors.initials: B
authors.lastname: Salisbury
authors.forename: R
authors.initials: R
authors.lastname: Sher
mesh_terms: D000818:Animals; D006224:Cricetinae; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008862:Microsomes, Liver / Q000201:enzymology; D051381:Rats; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D002785:Sterol O-Acyltransferase