Heterocyclic amides: Inhibitors of acyl-CoA: cholesterol O-acyl transferase with hypocholesterolemic activity in several species and antiatherosclerotic activity in the …

…, CF Purchase, JA Picard, MK Anderson…

文献索引：O'Brien; Sliskovic; Picard; Lee; Purchase II; Roth; White; Anderson; Mueller; Bocan; Bousley; Hamelehle; Homan; Krause; Reindel; Stanfield; Turluck Journal of Medicinal Chemistry, 1996 , vol. 39, # 12 p. 2354 - 2366

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被引用次数: 17

摘要

A series of heterocyclic amides were synthesized and evaluated as inhibitors of acyl-CoA: cholesterol O-acyltransferase (ACAT) in vitro and for cholesterol lowering in cholesterol-fed rats. Compounds were evaluated for cell-based macrophage ACAT inhibition, bioactivity, and adrenal toxicity. Candidates were selected for evaluation in cholesterol-fed dogs and, ultimately, the injured cholesterol-fed rabbit model of atherosclerosis. The heterocyclic ...