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Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond

✍ Scribed by Roark, W. Howard; Roth, Bruce D.; Holmes, Ann; Trivedi, Bharat K.; Kieft, Karen A.; Essenburg, Arnold D.; Krause, Brian R.; Stanfield, Richard L.


Book ID
124158347
Publisher
American Chemical Society
Year
1993
Tongue
English
Weight
790 KB
Volume
36
Category
Article
ISSN
0022-2623

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Inhibitors of acyl-CoA: cholesterol O-ac
✍ D.R. Sliskovic; J.A. Picard; W.H. Roark; A.D. Essenburg; B.R. Krause; L.L. Minto πŸ“‚ Article πŸ“… 1996 πŸ› Elsevier Science 🌐 English βš– 332 KB

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