INHIBITORS OF ACYL-COA - CHOLESTEROL O-ACYL TRANSFERASE (ACAT) AS HYPOCHOLESTEROLEMIC AGENTS - THE SYNTHESIS AND BIOLOGICAL-ACTIVITY OF A SERIES OF MALONESTER AMIDES

Authors
SLISKOVIC DR PICARD JA ROARK WH ESSENBURG AD KRAUSE BR MINTON LL REINDEL JF STANFIELD RL
Citation
Dr. Sliskovic et al., INHIBITORS OF ACYL-COA - CHOLESTEROL O-ACYL TRANSFERASE (ACAT) AS HYPOCHOLESTEROLEMIC AGENTS - THE SYNTHESIS AND BIOLOGICAL-ACTIVITY OF A SERIES OF MALONESTER AMIDES, Bioorganic & medicinal chemistry letters, 6(6), 1996, pp. 713-718
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
6
Year of publication
1996
Pages
713 - 718
Database
ISI
SICI code
0960-894X(1996)6:6<713:IOA-CO>2.0.ZU;2-L
Abstract
The synthesis and structure-activity relationships of a series of malo nester amide ACAT inhibitors are described. One of these compounds, 4s , was shown to be a potent inhibitor of both the intestinal and arteri al enzymes, bioactive upon oral dosing (ex vivo bioassay) and efficaci ous in a clinically relevant rodent model of preestablished hyperchole sterolemia.