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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2010-6-4
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pubmed:abstractText |
Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we synthesized 3,5-disubstituted-oxadiazoles and tetrazoles as mGluR5 NAMs. Based on the analysis of ligand efficiency and lipophilic efficiency metrics we identified a promising lead candidate as a starting point for further optimization.
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pubmed:commentsCorrections |
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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 |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BielikAttilaA,
pubmed-author:BobokAmritaA,
pubmed-author:DományGyörgyG,
pubmed-author:GálKrisztinaK,
pubmed-author:GreinerIstvánI,
pubmed-author:HorváthAttilaA,
pubmed-author:KeseruGyörgy MGM,
pubmed-author:KissBélaB,
pubmed-author:KolokSándorS,
pubmed-author:KurkóDalmaD,
pubmed-author:MolnárLászlóL,
pubmed-author:NógrádiKatalinK,
pubmed-author:NagyJózsefJ,
pubmed-author:NyékiOlgaO,
pubmed-author:SzombathelyiZsoltZ,
pubmed-author:WágnerGáborG,
pubmed-author:WéberCsabaC
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3737-41
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pubmed:dateRevised |
2011-8-1
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.
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pubmed:affiliation |
Gedeon Richter Plc, Budapest, Hungary. g.wagner@richter.hu
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pubmed:publicationType |
Journal Article
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