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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2008-10-20
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pubmed:abstractText |
Several novel classes of potent and small amide-type inhibitors of glycine transport (GlyT1) were developed through sequential simplification of a benzodiazepinone-lead structure identified from a high-throughput screening. The most potent compounds of these structurally simple classes show low nanomolar inhibition at the GlyT1 target.
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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 |
Oct
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5533-6
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pubmed:meshHeading |
pubmed-meshheading:18805008-Amides,
pubmed-meshheading:18805008-Animals,
pubmed-meshheading:18805008-Benzodiazepinones,
pubmed-meshheading:18805008-Chemistry, Pharmaceutical,
pubmed-meshheading:18805008-Drug Design,
pubmed-meshheading:18805008-Glycine Plasma Membrane Transport Proteins,
pubmed-meshheading:18805008-Humans,
pubmed-meshheading:18805008-Inhibitory Concentration 50,
pubmed-meshheading:18805008-Mice,
pubmed-meshheading:18805008-Microsomes,
pubmed-meshheading:18805008-Models, Chemical,
pubmed-meshheading:18805008-Permeability,
pubmed-meshheading:18805008-Solubility,
pubmed-meshheading:18805008-Stereoisomerism,
pubmed-meshheading:18805008-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
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pubmed:affiliation |
F. Hoffmann-La Roche Ltd., Pharmaceutical Research Basel, Discovery Chemistry, CH-4070 Basel, Switzerland. synese.jolidon@roche.com
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pubmed:publicationType |
Journal Article
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