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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2008-1-30
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pubmed:abstractText |
The CXCR2 SAR of a series of bicyclic antagonists such as the 2-aminothiazolo[4,5-d]pyrimidine 3b was investigated by systematic variation of the fused pyrimidine-based heterocyclic cores. Replacement of the aminothiazole ring with a 2-thiazolone alternative led to a series of thiazolo[4,5-d]pyrimidine-2(3H)-one antagonists with markedly improved biological and pharmacokinetic properties, which are suitable pharmacological tools to probe the in vivo effects of CXCR2 antagonism combined with the associated CCR2 activity.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AustinCarolineC,
pubmed-author:AustinRupertR,
pubmed-author:BonnertRogerR,
pubmed-author:CagePeterP,
pubmed-author:ChristieMarkM,
pubmed-author:David Nicholls,
pubmed-author:David Robinson,
pubmed-author:EbdenMarkM,
pubmed-author:GardinerStuartS,
pubmed-author:GrahamesCarolineC,
pubmed-author:HillStevenS,
pubmed-author:HuntFraserF,
pubmed-author:JewellRobertR,
pubmed-author:LewisShirleyS,
pubmed-author:MartinIainI,
pubmed-author:WaltersIainI
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
798-803
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pubmed:meshHeading |
pubmed-meshheading:18240390-Administration, Oral,
pubmed-meshheading:18240390-Animals,
pubmed-meshheading:18240390-Biological Availability,
pubmed-meshheading:18240390-Drug Evaluation, Preclinical,
pubmed-meshheading:18240390-Pyrimidines,
pubmed-meshheading:18240390-Rats,
pubmed-meshheading:18240390-Receptors, Interleukin-8B,
pubmed-meshheading:18240390-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Evaluation of a series of bicyclic CXCR2 antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, United Kingdom. iain.walters@astrazeneca.com
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pubmed:publicationType |
Journal Article
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