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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2009-9-2
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pubmed:abstractText |
Antagonists of the human A(2A) receptor have been reported to have potential therapeutic benefit in the alleviation of the symptoms associated with neurodegenerative movement disorders such as Parkinson's disease. As part of our efforts to discover potent and selective antagonists of this receptor, we herein describe the detailed optimization and structure-activity relationships of a series of pyrimidine-4-carboxamides. These optimized derivatives display desirable physiochemical and pharmacokinetic profiles, which have led to promising oral activity in clinically relevant models of Parkinson's disease.
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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 |
Sep
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:BamfordSamantha JSJ,
pubmed-author:ClayAlexA,
pubmed-author:GaurSuneelS,
pubmed-author:GillespieRoger JRJ,
pubmed-author:HaymesTimT,
pubmed-author:JacksonPhilip SPS,
pubmed-author:JordanAllan MAM,
pubmed-author:KlenkeBurkhardB,
pubmed-author:LeonardiStefaniaS,
pubmed-author:LiuJeanetteJ,
pubmed-author:MansellHoward LHL,
pubmed-author:QiaoJoeJ,
pubmed-author:SaadiMonaM,
pubmed-author:SimmoniteHeatherH,
pubmed-author:StrattonGemma CGC,
pubmed-author:ToddRichard SRS,
pubmed-author:WilliamsonDouglas SDS,
pubmed-author:YuleIan AIA
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6590-605
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:19695884-Adenosine A2 Receptor Antagonists,
pubmed-meshheading:19695884-Animals,
pubmed-meshheading:19695884-Humans,
pubmed-meshheading:19695884-Locomotion,
pubmed-meshheading:19695884-Mice,
pubmed-meshheading:19695884-Parkinson Disease,
pubmed-meshheading:19695884-Protein Binding,
pubmed-meshheading:19695884-Pyrimidines,
pubmed-meshheading:19695884-Receptor, Adenosine A2A,
pubmed-meshheading:19695884-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
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pubmed:affiliation |
Department of Chemistry, Vernalis (R&D) Ltd, 613 Reading Road, Winnersh, Wokingham RG41 5UA, UK.
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pubmed:publicationType |
Journal Article
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