rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2002-5-28
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pubmed:abstractText |
A series of substituted tetrahydrofuroyl-1-phenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. Substitution of the alpha carbon of the tetrahydrofuran with aryl groups increased the specificity for VLA-4 versus alpha(4)beta(7) while amide substitution increased the potency of the series without increasing the specificity. Substitution of the beta carbon of the tetrahydrofuran with keto or amino groups slightly improved the specificity for VLA-4 versus alpha(4)beta(7) but with a significant loss in binding affinity for VLA-4.
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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 |
Jun
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BorgesEditeE,
pubmed-author:ChangLinda LLL,
pubmed-author:DohertyGeorge AGA,
pubmed-author:EggerLinda ALA,
pubmed-author:HagmannWilliam KWK,
pubmed-author:KidambiUshaU,
pubmed-author:MacCossMalcolmM,
pubmed-author:McCauleyErmenegildaE,
pubmed-author:MumfordRichard ARA,
pubmed-author:SchmidtJohn AJA,
pubmed-author:TongSharonS,
pubmed-author:Van RiperGailG,
pubmed-author:YangGinger XGX
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pubmed:issnType |
Print
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pubmed:day |
3
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1501-5
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:12031329-Administration, Oral,
pubmed-meshheading:12031329-Animals,
pubmed-meshheading:12031329-Furans,
pubmed-meshheading:12031329-Humans,
pubmed-meshheading:12031329-Inhibitory Concentration 50,
pubmed-meshheading:12031329-Integrin alpha4beta1,
pubmed-meshheading:12031329-Ligands,
pubmed-meshheading:12031329-Molecular Weight,
pubmed-meshheading:12031329-Phenylalanine,
pubmed-meshheading:12031329-Rats,
pubmed-meshheading:12031329-Stereoisomerism,
pubmed-meshheading:12031329-Structure-Activity Relationship,
pubmed-meshheading:12031329-Substrate Specificity,
pubmed-meshheading:12031329-Sulfonamides,
pubmed-meshheading:12031329-Vascular Cell Adhesion Molecule-1
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pubmed:year |
2002
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pubmed:articleTitle |
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. george_doherty@merck.com
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pubmed:publicationType |
Journal Article
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