Inhibitors of acyl CoA:cholesterol acyltransferase.
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.
Vaccaro
W
W
Schering-Plough Research Institute, Kenilworth, New Jersey 07033-0539, USA.
Amore
C
C
Berger
J
J
Burrier
R
R
Clader
J
J
Davis
H
H
Domalski
M
M
Fevig
T
T
Salisbury
B
B
Sher
R
R
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
D004791:Enzyme Inhibitors; D002785:Sterol O-Acyltransferase