Source:http://linkedlifedata.com/resource/pubmed/id/21134748
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2010-12-24
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pubmed:abstractText |
Two complementary stereospecific synthetic approaches for the preparation of unsymmetrical ortho-substituted N-(4,4-diphenylbut-3-enyl) derivatives of nipecotic acid are described. Determination of the activity of the prepared compounds at the GAT-1 transporter highlighted differing SAR requirements of the E- and Z-phenyl rings, and led to the discovery of a compound with comparable potency to tiagabine. Some attempts to replace nipecotic acid with alternative novel amino acids are also described.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BernasconiGiovanniG,
pubmed-author:CarnevaleGennaroG,
pubmed-author:Di FabioRomanoR,
pubmed-author:FalchiAlessandroA,
pubmed-author:GrecoElisabettaE,
pubmed-author:LeslieColin PCP,
pubmed-author:MangiariniLauraL,
pubmed-author:NegriMicheleM,
pubmed-author:PizziDomenica ADA,
pubmed-author:SeriCatiaC,
pubmed-author:SquagliaMichelaM
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pubmed:copyrightInfo |
Copyright © 2010. Published by Elsevier Ltd.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
602-5
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pubmed:meshHeading |
pubmed-meshheading:21134748-GABA Plasma Membrane Transport Proteins,
pubmed-meshheading:21134748-GABA Uptake Inhibitors,
pubmed-meshheading:21134748-Nipecotic Acids,
pubmed-meshheading:21134748-Protein Binding,
pubmed-meshheading:21134748-Stereoisomerism,
pubmed-meshheading:21134748-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.
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pubmed:affiliation |
Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy. domenica.a.pizzi@gsk.com
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pubmed:publicationType |
Journal Article
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