Abstract
4-Aryl-1,8-naphthyridin-2(1H)-on-3-yl urea derivatives with hydrophilic groups were synthesized in order to improve aqueous solubility and pharmacokinetic property. SMP-797 possessing (4-aminophenyl)ureido and 3-(hydroxypropoxyphenyl) moieties showed potent ACAT inhibitory activity and excellent oral efficacy.
MeSH terms
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Acyltransferases / chemistry
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Administration, Oral
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Anticholesteremic Agents / chemistry
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Anticholesteremic Agents / pharmacology*
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Drug Design*
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Enzyme Inhibitors / pharmacology*
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Humans
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Hypercholesterolemia / drug therapy
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Structure
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Naphthyridines / chemistry*
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Naphthyridines / pharmacology*
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Solubility
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Sterol O-Acyltransferase / antagonists & inhibitors*
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Temperature
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Time Factors
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Urea / analogs & derivatives*
Substances
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Anticholesteremic Agents
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Enzyme Inhibitors
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Naphthyridines
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SMP-797
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Urea
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Acyltransferases
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Sterol O-Acyltransferase