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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 |
2005-5-24
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pubmed:abstractText |
Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6-6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa activity was detected in plasma of rats orally administered with 1mg/kg of compound 75b.
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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 |
0968-0896
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pubmed:author |
pubmed-author:FurugooriTaketoshiT,
pubmed-author:HaginoyaNoriyasuN,
pubmed-author:HorinoHaruhikoH,
pubmed-author:IsobeYumikoY,
pubmed-author:KobayashiShozoS,
pubmed-author:KomoriyaSatoshiS,
pubmed-author:MochizukiAkiyoshiA,
pubmed-author:NagaharaTakayasuT,
pubmed-author:NagataTsutomuT,
pubmed-author:SuzukiMakotoM,
pubmed-author:SuzukiMasanoriM,
pubmed-author:YoshinoToshiharuT
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pubmed:issnType |
Print
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pubmed:day |
2
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3927-54
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pubmed:meshHeading |
pubmed-meshheading:15911309-Administration, Oral,
pubmed-meshheading:15911309-Animals,
pubmed-meshheading:15911309-Anticoagulants,
pubmed-meshheading:15911309-Binding Sites,
pubmed-meshheading:15911309-Blood Coagulation,
pubmed-meshheading:15911309-Blood Coagulation Tests,
pubmed-meshheading:15911309-Drug Design,
pubmed-meshheading:15911309-Factor Xa,
pubmed-meshheading:15911309-Humans,
pubmed-meshheading:15911309-Intestinal Absorption,
pubmed-meshheading:15911309-Rats,
pubmed-meshheading:15911309-Serine Proteinase Inhibitors,
pubmed-meshheading:15911309-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites.
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pubmed:affiliation |
Tokyo R&D Center, Daiichi Pharmaceutical Co. Ltd, 16-13 Kita-Kasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan. komor0ni@daiichipharm.co.jp
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pubmed:publicationType |
Journal Article
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