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

✍ Scribed by D.R. Sliskovic; J.A. Picard; W.H. Roark; A.D. Essenburg; B.R. Krause; L.L. Minton; J.F. Reindel; R.L. Stanfield

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 332 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00098-4

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✦ Synopsis

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.

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