Inhibitors of Acyl CoA:Cholesterol Acyltransferase

详细信息    查看全文

• 作者：Wayne Vaccaro ; Cindy Amore ; Joel Berger ; Robert Burrier ; John Clader ; Harry Davis ; Martin Domalski ; Tom Fevig ; Brian Salisbury ; and Rosy Sher
• 刊名：Journal of Medicinal Chemistry
• 出版年：1996
• 出版时间：April 12, 1996
• 年：1996
• 卷：39
• 期：8
• 页码：1704 - 1719
• 全文大小：548K
• 年卷期：v.39,no.8(April 12, 1996)
• ISSN：1520-4804

文摘

Conformational restriction of previously disclosed acyclicdiphenylethyl)diphenylacetamidesled to the discovery of several potent inhibitors of acylCoA:cholesterol acyltransferase (ACAT).cis-[2-(4-Hydroxyphenyl)-1-indanyl]diphenylacetamide(4a) was the most potent ACAT inhibitoridentified (IC₅₀ = 0.04 M in an in vitrorat hepatic microsomal ACAT assay, ED₅₀ =0.72mg/kg/day in cholesterol-fed hamsters).