Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of …

PM O'Brien, DR Sliskovic, CJ Blankley…

文献索引：O'Brien; Sliskovic; Blankley; Roth; Wilson; Hamelehle; Krause; Stanfield Journal of Medicinal Chemistry, 1994 , vol. 37, # 12 p. 1810 - 1822

全文：HTML全文

被引用次数: 56

摘要

A series of disubstituted ureas containing amide or amine groups was prepared and evaluated for their ability to inhibit acyl-CoA: cholesterol O-acyl transferase in vitro and to lower plasma total cholesterol in a variety of cholesterol-fed rat models in vivo. The presence of polar or ionizable functionalities within this class of compounds may impart greater aqueous solubility to those compounds and thus allow improved transport to the enzyme ...