pubmed-article:18096386 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0026837 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0021467 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0184512 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C1413189 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C1527148 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0021469 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C1326501 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C1705542 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0439284 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C1880355 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0439596 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C2353870 | lld:lifeskim |
pubmed-article:18096386 | lifeskim:mentions | umls-concept:C0231517 | lld:lifeskim |
pubmed-article:18096386 | pubmed:issue | 2 | lld:pubmed |
pubmed-article:18096386 | pubmed:dateCreated | 2008-1-21 | lld:pubmed |
pubmed-article:18096386 | pubmed:abstractText | Conformational analysis of trans-1,2-disubstituted cyclohexane CCR3 antagonist 2 revealed that the cyclohexane linker could be replaced by an acyclic syn-alpha-methyl-beta-hydroxypropyl linker. Synthesis and biological evaluation of mono- and disubstituted propyl linkers support this conformational correlation. It was also found that the alpha-methyl group to the urea lowered protein binding and that the beta-hydroxyl group lowered affinity for CYP2D6. Ab initio calculations show that the alpha-methyl group governs the spatial orientation of three key functionalities within the molecule. alpha-Methyl-beta-hydroxypropyl urea 31 with a chemotaxis IC(50)=38 pM for eosinophils was chosen to enter clinical development for the treatment of asthma. | lld:pubmed |
pubmed-article:18096386 | pubmed:language | eng | lld:pubmed |
pubmed-article:18096386 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:18096386 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:18096386 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:18096386 | pubmed:month | Jan | lld:pubmed |
pubmed-article:18096386 | pubmed:issn | 1464-3405 | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:YaoWenqingW | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:DeciccoCarl... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:TebbenAndrew... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:DaviesPaulP | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:WackerDean... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:SantellaJosep... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:GardnerDaniel... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:DeLuccaGeorge... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:KoSoo SSS | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:WatsonPaul... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:WelchPatricia... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:WadmanEric... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:SolomonKimber... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:DunciaJohn... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:CarterPercy... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:KarivIlonaI | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:MandlekarSand... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:YeleswaramSwa... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:ShiChongsheng... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:ReddyPrabhaka... | lld:pubmed |
pubmed-article:18096386 | pubmed:author | pubmed-author:GradenDani... | lld:pubmed |
pubmed-article:18096386 | pubmed:issnType | Electronic | lld:pubmed |
pubmed-article:18096386 | pubmed:day | 15 | lld:pubmed |
pubmed-article:18096386 | pubmed:volume | 18 | lld:pubmed |
pubmed-article:18096386 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:18096386 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:18096386 | pubmed:pagination | 576-85 | lld:pubmed |
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pubmed-article:18096386 | pubmed:year | 2008 | lld:pubmed |
pubmed-article:18096386 | pubmed:articleTitle | From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis. | lld:pubmed |
pubmed-article:18096386 | pubmed:affiliation | Bristol-Myers Squibb Company, R&D, PO Box 4000, Princeton, NJ 08543-4000, USA. | lld:pubmed |
pubmed-article:18096386 | pubmed:publicationType | Journal Article | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:18096386 | lld:chembl |