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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
21
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pubmed:dateCreated |
1992-11-27
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pubmed:abstractText |
Substitution of hydroxy and hydroxyalkyl functionality at C-7 of the hexahydronaphthalene nucleus of simvastatin has provided novel analogs. The synthetic strategy employed epoxidation or Lewis acid-catalyzed aldol reaction of the 8-keto silyl enol ether as a key reactive intermediate. These analogs were evaluated as potential hypocholesterolemic agents via initial determination of their ability to inhibit HMG-CoA reductase in vitro. Oral activity of these compounds was determined in an acute rat model and a three-week study in cholestyramine-primed dogs. Compounds were identified that possessed in vitro and in vivo activity comparable to that of simvastatin.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
3813-21
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:1433193-Administration, Oral,
pubmed-meshheading:1433193-Animals,
pubmed-meshheading:1433193-Anticholesteremic Agents,
pubmed-meshheading:1433193-Disease Models, Animal,
pubmed-meshheading:1433193-Dogs,
pubmed-meshheading:1433193-Hydroxymethylglutaryl-CoA Reductase Inhibitors,
pubmed-meshheading:1433193-Hypercholesterolemia,
pubmed-meshheading:1433193-Lovastatin,
pubmed-meshheading:1433193-Magnetic Resonance Spectroscopy,
pubmed-meshheading:1433193-Rats,
pubmed-meshheading:1433193-Simvastatin,
pubmed-meshheading:1433193-Structure-Activity Relationship
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pubmed:year |
1992
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pubmed:articleTitle |
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.
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pubmed:affiliation |
Merck Research Laboratories, West Point, Pennsylvania 19486.
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pubmed:publicationType |
Journal Article
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