Heterocyclic Ureas: Inhibitors of Acyl-CoA: Cholesterol O-Acyltransferase as Hypocholesterolemic Agents 1

…, KL Hamelehle, BR Krause, RL Stanfield…

Index: White, Andrew D.; Creswell, Mark W.; Chucholowski, Alexander W.; Blankley, C. John; Wilson, Michael W.; Bousley, Richard F.; Essenburg, Arnold D.; Hamelehle, Katherine L.; Krause, Brian R.; Stanfield, Richard L.; Dominick, Mark A.; Neub, Martin Journal of Medicinal Chemistry, 1996 , vol. 39, # 22 p. 4382 - 4395

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Citation Number: 45

Abstract

A series of diaryl-substituted heterocyclic ureas was prepared, and their ability to inhibit acyl- CoA: cholesterol O-acyltransferase (ACAT) in vitro and to lower plasma total cholesterol in cholesterol-fed animal models in vivo was examined. N-(2, 6-Diisopropylphenyl)-N'-tetrazole- or isoxazole-substituted heterocyclic ureas proved optimal. A carbon chain of 11-14 carbons substituted 1, 3 with respect to the amine provided the optimal side chain. Substitution of ...