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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-9
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pubmed:abstractText |
The optimization of a series of 1-aryl-3-piperidinyl urea derivatives is described in which incorporation of tropenyl and homotropenyl moieties has led to significant improvements in activity and drug-like properties. Replacement of the central piperidine with an exo-tropanyl unit led to the identification of compound 15 which provides a combination of excellent potency against human and murine receptors, drug-like properties and pharmacokinetics, thus providing a valuable tool for the evaluation of CXCR3 antagonists in models of human 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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AllenDaniel RDR,
pubmed-author:BirchHelen LHL,
pubmed-author:ChapmanGayle AGA,
pubmed-author:GalvinFrances CFC,
pubmed-author:JoplingLouise ALA,
pubmed-author:KnightRoland LRL,
pubmed-author:MeierDoricaD,
pubmed-author:MeissnerJohannes W GJW,
pubmed-author:OliverKathrynK,
pubmed-author:OwenDavid ADA,
pubmed-author:ThomasElizabeth JEJ,
pubmed-author:TremayneNeilN,
pubmed-author:WatsonRobert JRJ,
pubmed-author:WilliamsSophie CSC
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pubmed:issnType |
Electronic
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pubmed:day |
1
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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 |
147-51
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pubmed:meshHeading |
pubmed-meshheading:18032038-Animals,
pubmed-meshheading:18032038-Cycloparaffins,
pubmed-meshheading:18032038-Humans,
pubmed-meshheading:18032038-Mice,
pubmed-meshheading:18032038-Mice, Inbred BALB C,
pubmed-meshheading:18032038-Models, Molecular,
pubmed-meshheading:18032038-Piperidines,
pubmed-meshheading:18032038-Receptors, CXCR3,
pubmed-meshheading:18032038-Urea
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pubmed:year |
2008
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pubmed:articleTitle |
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.
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pubmed:affiliation |
UCB Inflammation Discovery, Granta Park, Great Abington, Cambridge CB21 6GS, United Kingdom. bob.watson@ucb-group.com
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pubmed:publicationType |
Journal Article
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