Inhibitors of Acyl CoA:Cholesterol Acyltransferase

Vaccaro, Wayne; Amore, Cindy; Berger, Joel G.; Burrier, Robert E.; Clader, John W.; Davis, Harry R.; Domalski, Martin S.; Fevig, Tom; Salisbury, Brian; Sher, Rosy

doi:10.1021/jm950833d

Cited by 40 publications

(28 citation statements)

References 20 publications

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“…Because ACAT enzymes participate in cholesterol ester synthesis for assembly of atherogenic apoB-containing lipoproteins (59,60) and in macrophage foam cell formation, ACAT inhibitors have been developed as potential therapeutics (61)(62)(63)(64). These agents produced mixed results in several animal models.…”

Section: Acat and Dgat Enzymes As Pharmaceutical Targetsmentioning

confidence: 99%

The Enzymes of Neutral Lipid Synthesis

Buhman¹,

Chen²,

Farese³

2001

Journal of Biological Chemistry

151

115

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Section: Acat and Dgat Enzymes As Pharmaceutical Targetsmentioning

confidence: 99%

The Enzymes of Neutral Lipid Synthesis

Buhman¹,

Chen²,

Farese³

2001

Journal of Biological Chemistry

151

115

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“…Typically serum cholesterol (SC) levels were not significantly reduced by ACAT inhibitors in this model [6], although anilides such as 3 [7] were a frequent exception. The first azetidinone CAI, 4, Fig.…”

Section: Discovery Of Azetidinone Caismentioning

confidence: 75%

Ezetimibe and other Azetidinone Cholesterol Absorption Inhibitors

Clader¹

2005

CTMC

Self Cite

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Atherosclerotic coronary artery disease remains a major healthcare concern especially in developed countries. While lowering plasma cholesterol levels via diet, exercise, and pharmacotherapy can reduce this risk of developing coronary artery disease, there remains a need for more effective drug therapies. The azetidinone cholesterol absorption inhibitors typified by ezetimibe represent the first new approach to lipid lowering therapy in more than a decade. This review summarizes the medicinal chemistry of the azetidinone cholesterol absorption inhibitors as a class, with emphasis on factors that contributed both to the discovery of ezetimibe as well as to our overall understanding of S.A.R. trends in this area.

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“…Vaccaro et al have prepared various 2-Azetidinone derivatives as Cholesterol Absorption Inhibitors [56]. Cholesterol absorption inhibition was assessed in orally dosed, cholesterol-fed hamsters as reported in literature.…”

Section: Mm)mentioning

confidence: 99%