Inhibitors of Acyl CoA:Cholesterol Acyltransferase
Journal of Medicinal Chemistry1996Vol. 39(8), pp. 1704–1719
Citations Over TimeTop 11% of 1996 papers
Wayne Vaccaro, Cindy Amore, Joel G. Berger, Robert E. Burrier, John W. Clader, Harry R. Davis, Martin S. Domalski, Tom Fevig, Brian Salisbury, Rosy Sher
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.
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