rdf:type |
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lifeskim:mentions |
|
pubmed:issue |
17
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pubmed:dateCreated |
2002-8-8
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pubmed:abstractText |
Structure-activity relationship (SAR) studies of initial screening hits from our corporate library of compounds and a structurally related series of CCR1 receptor antagonists were used to determine that an N-(alkyl)benzylpiperidine is an essential pharmacophore for selective CCR3 antagonists. Further SAR studies that introduced N-(ureidoalkyl) substituents improved the binding potency of these compounds from the micromolar to the low nanomolar range. This new series of compounds also displays highly potent, in vitro functional CCR3-mediated antagonism of eotaxin-induced Ca(2+) mobilization and chemotaxis of human eosinophils.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Allergic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/CCL11 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/CCR3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Chemokine CCL11,
http://linkedlifedata.com/resource/pubmed/chemical/Chemokines, CC,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, CCR3,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Chemokine,
http://linkedlifedata.com/resource/pubmed/chemical/Urea
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:CovingtonMaryanneM,
pubmed-author:DaviesPaulP,
pubmed-author:De LuccaGeorge VGV,
pubmed-author:DeciccoCarl PCP,
pubmed-author:JohnsonCurtC,
pubmed-author:KimUi TUT,
pubmed-author:KoSoo SSS,
pubmed-author:NewtonRobert CRC,
pubmed-author:SolomonKimberly AKA,
pubmed-author:TrainorGeorge LGL,
pubmed-author:VargoBrian JBJ,
pubmed-author:WelchPatricia KPK
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pubmed:issnType |
Print
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pubmed:day |
15
|
pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3794-804
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:12166951-Animals,
pubmed-meshheading:12166951-Anti-Allergic Agents,
pubmed-meshheading:12166951-CHO Cells,
pubmed-meshheading:12166951-Calcium,
pubmed-meshheading:12166951-Chemokine CCL11,
pubmed-meshheading:12166951-Chemokines, CC,
pubmed-meshheading:12166951-Chemotaxis, Leukocyte,
pubmed-meshheading:12166951-Cricetinae,
pubmed-meshheading:12166951-Eosinophils,
pubmed-meshheading:12166951-Humans,
pubmed-meshheading:12166951-Piperidines,
pubmed-meshheading:12166951-Receptors, CCR3,
pubmed-meshheading:12166951-Receptors, Chemokine,
pubmed-meshheading:12166951-Structure-Activity Relationship,
pubmed-meshheading:12166951-Urea
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pubmed:year |
2002
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pubmed:articleTitle |
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.
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pubmed:affiliation |
Bristol-Myers Squibb Company, Experimental Station, Wilmington, Delaware 19880-0336, USA. george.delucca@bms.com
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pubmed:publicationType |
Journal Article,
In Vitro
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