rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
1999-1-28
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pubmed:abstractText |
The design of a series of thromboxane receptor antagonists based on 3-(2-[[(4-chlorophenyl)sulfonyl]amino]ethyl)benzenepropanoic acid (1) is described. Addition of an arylmethyl group at the 5-position of 1 gave exceptionally potent agents in vitro and in vivo, with 13a (UK-147,535) giving complete blockade of the TxA2 receptor for greater than 12 hours in dogs, following an oral dose of 0.1 mg/kg.
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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 |
Aug
|
pubmed:issn |
0960-894X
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
18
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2061-6
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:9873486-15-Hydroxy-11 alpha,9...,
pubmed-meshheading:9873486-Animals,
pubmed-meshheading:9873486-Dogs,
pubmed-meshheading:9873486-Drug Design,
pubmed-meshheading:9873486-Indicators and Reagents,
pubmed-meshheading:9873486-Molecular Structure,
pubmed-meshheading:9873486-Phenylpropionates,
pubmed-meshheading:9873486-Platelet Aggregation,
pubmed-meshheading:9873486-Platelet Aggregation Inhibitors,
pubmed-meshheading:9873486-Receptors, Thromboxane,
pubmed-meshheading:9873486-Structure-Activity Relationship
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pubmed:year |
1998
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pubmed:articleTitle |
Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[[(4-chlorophenyl)sulfonyl]-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists.
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pubmed:affiliation |
Department of Discovery Chemistry, Pfizer Central Research, Sandwich, Kent, U.K. Kevin_Dack@sandwich.pfizer.com
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pubmed:publicationType |
Journal Article
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