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...

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Veröffentlicht in:	Journal of medicinal chemistry 1996-04, Vol.39 (8), p.1704-1719
Hauptverfasser:	Vaccaro, Wayne, Amore, Cindy, Berger, Joel, Burrier, Robert, Clader, John, Davis, Harry, Domalski, Martin, Fevig, Tom, Salisbury, Brian, Sher, Rosy
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cricetinae Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins Medical sciences Microsomes, Liver - enzymology Pharmacology. Drug treatments Rats Sterol O-Acyltransferase - antagonists & inhibitors Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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 μM in an in vitro rat hepatic microsomal ACAT assay, ED50 = 0.72 mg/kg/day in cholesterol-fed hamsters).
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm950833d