130804-30-7Relevant academic research and scientific papers
Mono- or diphenylpyridazines connected to N-(2,4-difluorophenyl)-N′- heptylurea as Acyl-CoA:cholesterol acyltransferase inhibitors
Gelain, Arianna,Bettinelli, Ilaria,Barlocco, Daniela,Kwon, Byoung-Mog,Jeong, Tae-Sook,Cho, Kyung-Hyun,Toma, Lucio
, p. 7708 - 7713 (2007/10/03)
Mono- and diphenylpyridazine ureido derivatives, structurally related to DuP 128, were synthesized and tested for their inhibitory activity against ACAT isolated from rat liver microsomes. Several compounds displayed ACAT inhibition in the micromolar range. The amino derivatives 4a-c were also tested against hACAT-1 and hACAT-2 isoforms. They retained the same trend shown in the previous assay. Modeling studies on representative terms were performed. Significant similarities between the geometrical features of the model DuP 128 and the most active pyridazine derivatives were observed.
Pyridazine derivatives as novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors
Gelain, Arianna
, p. 395 - 400 (2007/10/03)
Acyl-CoA:cholesterol acyltransferase (E.C.2.3.1.26, ACAT) is a microsomial enzyme that catalyses the formation of cholesteryl esters by acylation of cholesterol with long chain fatty acylCoA [1]. ACAT plays important roles in cellular homeostasis and in t
Design, Synthesis, and Structure-Activity Relationship Studies for a New Imidazole Series of J774 Macrophage Specific Acyl-CoA:Cholesterol Acyltransferase (ACAT) Inhibitors
Maduskuie, Thomas P.,Wilde, Richard G.,Billheimer, Jeffrey T.,Cromley, Debra A.,Germain, Sandra,et al.
, p. 1067 - 1083 (2007/10/02)
Acyl-CoA:cholesterol acyltransferase (ACAT) is the primary enzyme involved in intracellular cholesterol esterification.Arterial wall infiltration by macrophages and subsequent uncontrolled esterification of cholesterol leading to foam cell formation is believed to be an important process which leads to the development of fatty streaks.Inhibitors of the ACAT enzyme may retard this atherogenic process.We have recently discovered a series of imidazoles which are potent in vitro ACAT inhibitors in the J774 macrophage cell culture assay.This paper will describe the design, synthesis, and structure-activity relationship for this very potent series of compounds.
Fused-ring heterocycles for the treatment of atherosclerosis
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, (2008/06/13)
This invention relates to pyrazolo pyrimidines for the treatment of atherosclerosis as inhibitors of acyl--CoA, cholesterol acyetransferase (ACAT), and their use as antihypercholesterolemic agents, pharmaceutical compositions and preparation, and having t
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: Synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles
Higley,Wilde,Maduskuie,Johnson,Pennev,Billheimer,Robinson,Gillies,Wexler
, p. 3511 - 3522 (2007/10/02)
A series of 4,5-diaryl-2-(substituted thio)-1H-imidazoles has been synthesized and demonstrated to be potent inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). The design, synthesis, and structure-activity relationships for this series are reporte
Benzimidazoles for the treatment of atherosclerosis
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, (2008/06/13)
This invention relates to imidazoles, namely, fused-ring heterocycles as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), pharmaceutical compositions containing them, processes for their preparation, and their use as antihypercholesterolemic an
Use of imidazoles for the treatment of atherosclerosis
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, (2008/06/13)
This invention relates to imidazoles as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), processes for their preparation, and their use as antihypercholesterolemic agents or antiatherosclerotic. The compounds for use in the described method are
