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…

Index: 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

Full Text: HTML

Citation Number: 17

Abstract

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 ...

Related Articles:

Synthesis of (Z)-tetradec-11-en-1-ol and (Z)-hexadec-11-en-1-ol from dodecane-1, 12-diol

[Zakharkin, L. I.; Guseva, V. V. Chemistry of Natural Compounds, 1984 , vol. 20, # 6 p. 733 - 736 Khimiya Prirodnykh Soedinenii, 1984 , vol. 20, # 6 p. 776 - 779]

Synthesis of (Z)-tetradec-11-en-1-ol and (Z)-hexadec-11-en-1-ol from dodecane-1, 12-diol

[Zakharkin, L. I.; Guseva, V. V. Chemistry of Natural Compounds, 1984 , vol. 20, # 6 p. 733 - 736 Khimiya Prirodnykh Soedinenii, 1984 , vol. 20, # 6 p. 776 - 779]

Synthesis of γ, δ-Unsaturated-β-keto Lactones via Sequential Cross Metathesis-Lactonization: A Facile Entry to Macrolide Antibiotic (-)-A26771B

[Gebauer, Julian; Blechert, Siegfried Journal of Organic Chemistry, 2006 , vol. 71, # 5 p. 2021 - 2025]

Synthesis of γ, δ-Unsaturated-β-keto Lactones via Sequential Cross Metathesis-Lactonization: A Facile Entry to Macrolide Antibiotic (-)-A26771B

[Gebauer, Julian; Blechert, Siegfried Journal of Organic Chemistry, 2006 , vol. 71, # 5 p. 2021 - 2025]

Design, chemical synthesis, and in vitro biological evaluation of simplified estradiol-adenosine hybrids as inhibitors of 17β-hydroxysteroid dehydrogenase type 1

[Berube, Marie; Poirier, Donald Canadian Journal of Chemistry, 2009 , vol. 87, # 8 p. 1180 - 1199]

More Articles...