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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2009-3-9
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pubmed:abstractText |
The purinoceptor subtypes P2X(3) and P2X(2/3) have been shown to play a pivotal role in models of various pain conditions. Identification of a potent and selective dual P2X(3)/P2X(2/3) diaminopyrimidine antagonist RO-4 prompted subsequent optimization of the template. This paper describes the SAR and optimization of the diaminopyrimidine ring and particularly the substitution of the 2-amino group. The discovery of the highly potent and drug-like dual P2X(3)/P2X(2/3) antagonist RO-51 is presented.
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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 |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AlamMuzaffarM,
pubmed-author:BoisDaisy Joe DuDJ,
pubmed-author:CarterDavid SDS,
pubmed-author:DillonMichael PMP,
pubmed-author:FordAnthony P D WAP,
pubmed-author:GeverJoel RJR,
pubmed-author:JahangirAlamA,
pubmed-author:LinClaraC,
pubmed-author:WagnerPaul JPJ,
pubmed-author:ZhaiYanshengY,
pubmed-author:ZiraJeffJ
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
1632-5
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:19231178-Adenosine Triphosphate,
pubmed-meshheading:19231178-Analgesics,
pubmed-meshheading:19231178-Animals,
pubmed-meshheading:19231178-CHO Cells,
pubmed-meshheading:19231178-Chemistry, Pharmaceutical,
pubmed-meshheading:19231178-Cricetinae,
pubmed-meshheading:19231178-Cricetulus,
pubmed-meshheading:19231178-Drug Design,
pubmed-meshheading:19231178-Drug Evaluation, Preclinical,
pubmed-meshheading:19231178-Humans,
pubmed-meshheading:19231178-Inhibitory Concentration 50,
pubmed-meshheading:19231178-Models, Chemical,
pubmed-meshheading:19231178-Pain,
pubmed-meshheading:19231178-Purinergic P2 Receptor Antagonists,
pubmed-meshheading:19231178-Pyrimidines,
pubmed-meshheading:19231178-Receptors, Purinergic P2,
pubmed-meshheading:19231178-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
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pubmed:affiliation |
Department of Medicinal Chemistry, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA.
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pubmed:publicationType |
Journal Article
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