Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. The synthesis and biological activity of a series of malonester amides

…, BR Krause, LL Minton, JF Reindel, RL Stanfield

Index: Sliskovic; Picard; Roark; Essenburg; Krause; Minton; Reindel; Stanfield Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 6 p. 713 - 718

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Citation Number: 12

Abstract

The synthesis and structure-activity relationships of a series of malonester amide ACAT inhibitors are described. One of these compounds, 4s, was shown to be a potent inhibitor of both the intestinal and arterial enzymes, bioactive upon oral dosing (ex vivo bioassay) and efficacious in a clinically relevant rodent model of preestablished hypercholesterolemia.