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rdf:type |
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lifeskim:mentions |
umls-concept:C0040018,
umls-concept:C0205177,
umls-concept:C0205531,
umls-concept:C0205681,
umls-concept:C0226896,
umls-concept:C0439849,
umls-concept:C0442027,
umls-concept:C1143778,
umls-concept:C1521991,
umls-concept:C1522538,
umls-concept:C1527415,
umls-concept:C1707689,
umls-concept:C1999216
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pubmed:issue |
1
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pubmed:dateCreated |
2001-12-12
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pubmed:abstractText |
A series of structurally novel small molecule inhibitors of human alpha-thrombin was prepared to elucidate their structure-activity relationships (SARs), selectivity and activity in vivo. BMS-189664 (3) is identified as a potent, selective, and orally active reversible inhibitor of human alpha-thrombin which is efficacious in vivo in a mouse lethality model, and at inhibiting both arterial and venous thrombosis in cynomolgus monkey models.
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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 |
0960-894X
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pubmed:author |
pubmed-author:ChangChiehying YCY,
pubmed-author:ChongSaehoS,
pubmed-author:DasJagabandhuJ,
pubmed-author:HallSteven ESE,
pubmed-author:HanWen ChingWC,
pubmed-author:IwanowiczEdwinE,
pubmed-author:KimballS DavidSD,
pubmed-author:LinJamesJ,
pubmed-author:MalleyMary FMF,
pubmed-author:MoquinRobert VRV,
pubmed-author:OgletreeMartin LML,
pubmed-author:ReidJoyce AJA,
pubmed-author:RobertsDaniel G MDG,
pubmed-author:SackJohn SJS,
pubmed-author:SchumacherWilliam AWA,
pubmed-author:SeilerSteven MSM,
pubmed-author:Wang-IversonDavid BDB
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pubmed:issnType |
Print
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pubmed:day |
7
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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 |
45-9
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:11738570-Administration, Oral,
pubmed-meshheading:11738570-Animals,
pubmed-meshheading:11738570-Binding Sites,
pubmed-meshheading:11738570-Crystallography, X-Ray,
pubmed-meshheading:11738570-Dipeptides,
pubmed-meshheading:11738570-Disease Models, Animal,
pubmed-meshheading:11738570-Dogs,
pubmed-meshheading:11738570-Drug Design,
pubmed-meshheading:11738570-Drug Evaluation, Preclinical,
pubmed-meshheading:11738570-Fibrinolytic Agents,
pubmed-meshheading:11738570-Humans,
pubmed-meshheading:11738570-Inhibitory Concentration 50,
pubmed-meshheading:11738570-Macaca fascicularis,
pubmed-meshheading:11738570-Mice,
pubmed-meshheading:11738570-Serine Proteinase Inhibitors,
pubmed-meshheading:11738570-Structure-Activity Relationship,
pubmed-meshheading:11738570-Sulfonamides,
pubmed-meshheading:11738570-Thrombin,
pubmed-meshheading:11738570-Thrombosis
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pubmed:year |
2002
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pubmed:articleTitle |
Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.
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pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. jagabandhu.das@bms.com
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pubmed:publicationType |
Journal Article
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