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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-3
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pubmed:abstractText |
In light of accumulating evidence that aggressive LDL-lowering therapy may offer increased protection against coronary heart disease, we undertook the design and synthesis of a novel series of HMG-CoA reductase inhibitors based upon a substituted pyrazole template. Optimizing this series using both structure-based design and molecular property considerations afforded a class of highly efficacious and hepatoselective inhibitors resulting in the identification of (3 R,5 R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2 H-pyrazol-3-yl]-3,5-dihydroxy-heptanoic (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
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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 |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AskewValerieV,
pubmed-author:AuerbachBruceB,
pubmed-author:BainbridgeGraemeG,
pubmed-author:CaspersNicoleN,
pubmed-author:ChoiChulhoC,
pubmed-author:DillonLisaL,
pubmed-author:HanselmanJeffrey CJC,
pubmed-author:HarrisMelissa SMS,
pubmed-author:HutchingsRichardR,
pubmed-author:KowalaMarkM,
pubmed-author:LarsenScott DSD,
pubmed-author:LinZhiwuZ,
pubmed-author:LuGina HGH,
pubmed-author:ParkWilliamW,
pubmed-author:PavlovskyAlexanderA,
pubmed-author:PfefferkornJeffrey AJA,
pubmed-author:RobertsonAndrewA,
pubmed-author:SekerkeCatherineC,
pubmed-author:TaitBradley DBD
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
31-45
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pubmed:meshHeading |
pubmed-meshheading:18072721-Animals,
pubmed-meshheading:18072721-Cholesterol, LDL,
pubmed-meshheading:18072721-Cricetinae,
pubmed-meshheading:18072721-Guinea Pigs,
pubmed-meshheading:18072721-Hepatocytes,
pubmed-meshheading:18072721-Heptanoic Acids,
pubmed-meshheading:18072721-Hydroxymethylglutaryl-CoA Reductase Inhibitors,
pubmed-meshheading:18072721-Hypercholesterolemia,
pubmed-meshheading:18072721-Liver,
pubmed-meshheading:18072721-Male,
pubmed-meshheading:18072721-Mesocricetus,
pubmed-meshheading:18072721-Muscle Cells,
pubmed-meshheading:18072721-Pyrazoles,
pubmed-meshheading:18072721-Rats,
pubmed-meshheading:18072721-Stereoisomerism,
pubmed-meshheading:18072721-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia.
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pubmed:affiliation |
Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, Michigan 48105, USA. jeffrey.a.pfefferkorn@pfizer.com
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pubmed:publicationType |
Journal Article,
In Vitro
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