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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2002-5-31
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pubmed:abstractText |
Based on DuPont Pharmaceuticals' monobenzamidine lead structure SN429, we have designed the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as a novel series of non-basic factor Xa inhibitors. We have discovered that the displacement of the benzamidine moiety with substituted 2-naphthyl structures not only results in highly potent factor Xa inhibitors, but also significantly increases their enzyme specificity and oral bioavailability.
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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 |
Jun
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:GoldmanErickE,
pubmed-author:HuangBrianB,
pubmed-author:HuangWenrongW,
pubmed-author:JiaZhaozhong JZJ,
pubmed-author:ParkGaryG,
pubmed-author:ReedAndreaA,
pubmed-author:ScarboroughRobert MRM,
pubmed-author:SinhaUmaU,
pubmed-author:WongPaulP,
pubmed-author:WoolfreyJohnJ,
pubmed-author:WuYanhongY,
pubmed-author:ZhangPenglieP,
pubmed-author:ZhuBing-YanBY
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pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1651-5
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
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pubmed:year |
2002
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pubmed:articleTitle |
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.
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pubmed:affiliation |
Medicinal Chemistry Department, Millennium Pharmaceuticals, Inc., 256 East Grand Ave, South San Francisco, CA 94080, USA. zhaozhong.jia@mpi.com
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pubmed:publicationType |
Journal Article
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