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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2009-4-17
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pubmed:abstractText |
The discovery, synthesis and SAR of a novel series of 3-benzyl-1,3-oxazolidin-2-ones as positive allosteric modulators (PAMs) of mGluR2 is described. Expedient hit-to-lead work on a single HTS hit led to the identification of a ligand-efficient and structurally attractive series of mGluR2 PAMs. Human microsomal clearance and suboptimal physicochemical properties of the initial lead were improved to give potent, metabolically stable and orally available mGluR2 PAMs.
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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 |
May
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:CandlerJohnJ,
pubmed-author:DoranAngela CAC,
pubmed-author:DuplantierAllen JAJ,
pubmed-author:EfremovIvanI,
pubmed-author:GanongAlan HAH,
pubmed-author:HaasJessica AJA,
pubmed-author:HanksAshley NAN,
pubmed-author:KrausKenneth GKG,
pubmed-author:LazzaroJohn TJTJr,
pubmed-author:LuJieminJ,
pubmed-author:MakladNohaN,
pubmed-author:McCarthySheryl ASA,
pubmed-author:O'SullivanTheresa JTJ,
pubmed-author:RogersBruce NBN,
pubmed-author:SiuciakJudith AJA,
pubmed-author:SpracklinDouglas KDK,
pubmed-author:ZhangLeiL
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2524-9
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pubmed:meshHeading |
pubmed-meshheading:19328692-Administration, Oral,
pubmed-meshheading:19328692-Allosteric Regulation,
pubmed-meshheading:19328692-Allosteric Site,
pubmed-meshheading:19328692-Carbamates,
pubmed-meshheading:19328692-Chemistry, Pharmaceutical,
pubmed-meshheading:19328692-Drug Design,
pubmed-meshheading:19328692-Humans,
pubmed-meshheading:19328692-Inhibitory Concentration 50,
pubmed-meshheading:19328692-Ligands,
pubmed-meshheading:19328692-Microsomes,
pubmed-meshheading:19328692-Models, Chemical,
pubmed-meshheading:19328692-Molecular Structure,
pubmed-meshheading:19328692-Oxazolidinones,
pubmed-meshheading:19328692-Receptors, Metabotropic Glutamate,
pubmed-meshheading:19328692-Schizophrenia
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pubmed:year |
2009
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pubmed:articleTitle |
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
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pubmed:affiliation |
CNS Chemistry, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA.
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pubmed:publicationType |
Journal Article
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