Abstract
The discovery that a series of N,N-dialkyl-N'-arylureas were inhibitors of the ACAT enzyme has led to a structure-activity study involving the systematic modification of three sites of the urea backbone. This study culminated in the selection of N'-(2,4-dimethylphenyl)-N-benzyl-N-n-butylurea (115) for more extensive biological evaluation. ACAT inhibitors are seen as potentially beneficial agents against hypercholesterolemia and atherosclerosis.
MeSH terms
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Adrenal Glands / enzymology
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Animals
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Anticholesteremic Agents / chemical synthesis*
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Aorta, Thoracic / enzymology
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Arteriosclerosis / prevention & control*
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Cells, Cultured
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Chlorocebus aethiops
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Diet, Atherogenic
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Liver / drug effects
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Liver / metabolism
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Male
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Molecular Structure
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Muscle, Smooth, Vascular / enzymology
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Rabbits
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Rats
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Sterols / metabolism
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Structure-Activity Relationship
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Urea / analogs & derivatives*
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Urea / chemical synthesis
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Urea / pharmacology
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Urea / therapeutic use
Substances
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Anticholesteremic Agents
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Sterols
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Urea
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Sterol O-Acyltransferase