Source:http://linkedlifedata.com/resource/pubmed/id/20097073
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2010-2-15
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pubmed:abstractText |
A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent agonists of the human TGR5 G-protein-coupled receptor is described. Many analogues were readily accessible via solution-phase synthesis which resulted in the rapid identification of key structure-activity relationships (SAR), and the discovery of potent exemplars (up to pEC50=9). Details of the SAR and optimization of this series are presented herein.
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1363-7
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pubmed:meshHeading |
pubmed-meshheading:20097073-Acrylamides,
pubmed-meshheading:20097073-Drug Design,
pubmed-meshheading:20097073-Humans,
pubmed-meshheading:20097073-Isoxazoles,
pubmed-meshheading:20097073-Molecular Structure,
pubmed-meshheading:20097073-Receptors, G-Protein-Coupled,
pubmed-meshheading:20097073-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.
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pubmed:affiliation |
Discovery Medicinal Chemistry, Discovery Research, GlaxoSmithKline Pharmaceuticals, 1250 South Collegeville Road, PO Box 5089, Collegeville, PA 19426-0989, USA.
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pubmed:publicationType |
Journal Article
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