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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
1996-8-26
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pubmed:abstractText |
The novel compound NO-1886, 4-[(diethoxyphosphoryl)methyl]-N-(4-bromo-2-cyanophenyl)-ben zamide, is a hypolipidemic agent, which appears to increase lipoprotein lipase activity in rats. Various analogs of NO-1886 were synthesized to study the structure-activity relationship of this hypolipidemic drug. A novel series of quinazolines and 4(3H)-quinazolinones were prepared by cyclization of NO-1886 derivatives. Derivatives bearing a 4-[(diethoxyphosphoryl)-methyl]phenyl] group at the 2-position were found to lower triglyceride and total cholesterol levels. In accord with the decrease in log P*, quinazolines and 4(3H)-quinazolinones showed good absorption and hypolipidemic activity. When the quinazolinone ring system is substituted at positions 6 and 7 with methoxy groups, increased hypolipidemic activity was observed. The highest hypolipidemic activity was observed when the 3-position was substituted by a methyl or benzyl group.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
29
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pubmed:volume |
39
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|
pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1433-7
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:8691473-Animals,
pubmed-meshheading:8691473-Arteriosclerosis,
pubmed-meshheading:8691473-Benzamides,
pubmed-meshheading:8691473-Biological Availability,
pubmed-meshheading:8691473-Cholesterol,
pubmed-meshheading:8691473-Chromatography, High Pressure Liquid,
pubmed-meshheading:8691473-Hyperlipidemias,
pubmed-meshheading:8691473-Hypolipidemic Agents,
pubmed-meshheading:8691473-Magnetic Resonance Spectroscopy,
pubmed-meshheading:8691473-Molecular Structure,
pubmed-meshheading:8691473-Organophosphorus Compounds,
pubmed-meshheading:8691473-Polyethylene Glycols,
pubmed-meshheading:8691473-Quinazolines,
pubmed-meshheading:8691473-Rats,
pubmed-meshheading:8691473-Rats, Sprague-Dawley,
pubmed-meshheading:8691473-Structure-Activity Relationship,
pubmed-meshheading:8691473-Triglycerides
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pubmed:year |
1996
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pubmed:articleTitle |
Synthesis and hypolipidemic activities of novel 2-[4-[diethoxyphosphoryl)methyl]phenyl]quinazolines and 4(3H)-quinazolinones.
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pubmed:affiliation |
Nutrition Research Institute, Otsuka Pharmaceutical Factory, Inc., Tokushima, Japan.
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pubmed:publicationType |
Journal Article
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