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pubmed-article:21134748pubmed:abstractTextTwo 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.lld:pubmed
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pubmed-article:21134748pubmed:authorpubmed-author:CarnevaleGenn...lld:pubmed
pubmed-article:21134748pubmed:copyrightInfoCopyright © 2010. Published by Elsevier Ltd.lld:pubmed
pubmed-article:21134748pubmed:issnTypeElectroniclld:pubmed
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pubmed-article:21134748pubmed:articleTitleStereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.lld:pubmed
pubmed-article:21134748pubmed:affiliationNeurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy. domenica.a.pizzi@gsk.comlld:pubmed
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