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rdf:type |
|
|
lifeskim:mentions |
|
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pubmed:issue |
8
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pubmed:dateCreated |
2009-4-3
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pubmed:abstractText |
A series of heterocyclic sulfonamides have been developed which are potent and selective inhibitors of hGlyT1. SAR studies to optimise the in vitro and in vivo properties are described. Optimisation of the central scaffold resulted in cyclohexane sulfones 28 and 29, which have good PK properties and show promise for further development.
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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 |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BlackabyWesley PWP,
pubmed-author:BrownTerry ATA,
pubmed-author:GoodacreSimon CSC,
pubmed-author:JenningsAndrew S RAS,
pubmed-author:LewisRichard TRT,
pubmed-author:PikeAndrewA,
pubmed-author:PillaiGopalanG,
pubmed-author:SmithAlisonA,
pubmed-author:StreetLeslie JLJ,
pubmed-author:ThomasSteveS,
pubmed-author:ThomsonJoanne LJL
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pubmed:issnType |
Electronic
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pubmed:day |
15
|
|
pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
|
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pubmed:pagination |
2235-9
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pubmed:meshHeading |
pubmed-meshheading:19318248-Administration, Oral,
pubmed-meshheading:19318248-Animals,
pubmed-meshheading:19318248-Biological Availability,
pubmed-meshheading:19318248-Glycine Plasma Membrane Transport Proteins,
pubmed-meshheading:19318248-Humans,
pubmed-meshheading:19318248-Male,
pubmed-meshheading:19318248-Microsomes, Liver,
pubmed-meshheading:19318248-Rats,
pubmed-meshheading:19318248-Rats, Sprague-Dawley,
pubmed-meshheading:19318248-Sulfonamides,
pubmed-meshheading:19318248-Triazoles
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pubmed:year |
2009
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pubmed:articleTitle |
Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Sharp and Dohme, Neuroscience Research Centre, Harlow, Essex, UK.
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pubmed:publicationType |
Journal Article,
Comparative Study
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