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rdf:type |
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lifeskim:mentions |
umls-concept:C0086418,
umls-concept:C0205177,
umls-concept:C0205531,
umls-concept:C0220825,
umls-concept:C0226896,
umls-concept:C0442027,
umls-concept:C0914069,
umls-concept:C1174038,
umls-concept:C1527415,
umls-concept:C1880355,
umls-concept:C1999216
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pubmed:issue |
18
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pubmed:dateCreated |
2002-8-16
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pubmed:abstractText |
The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man.
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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 |
Sep
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BlackieJosie AJA,
pubmed-author:BloomerJackie CJC,
pubmed-author:BrownMurray J BMJ,
pubmed-author:ChengHung-YuanHY,
pubmed-author:ElliottRichard LRL,
pubmed-author:HammondBeverleyB,
pubmed-author:HickeyDeirdre M BDM,
pubmed-author:IfeRobert JRJ,
pubmed-author:LeachColin ACA,
pubmed-author:LewisV AnnVA,
pubmed-author:MacpheeColin HCH,
pubmed-author:MillinerKevin JKJ,
pubmed-author:MooresKitty EKE,
pubmed-author:PintoIvan LIL,
pubmed-author:SmithStephen ASA,
pubmed-author:StansfieldIan GIG,
pubmed-author:StanwaySteven JSJ,
pubmed-author:TaylorMaxine AMA,
pubmed-author:TheobaldColin JCJ,
pubmed-author:WhittakerCaroline MCM
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pubmed:issnType |
Print
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pubmed:day |
16
|
|
pubmed:volume |
12
|
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pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
2603-6
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:12182870-Administration, Oral,
pubmed-meshheading:12182870-Animals,
pubmed-meshheading:12182870-Biphenyl Compounds,
pubmed-meshheading:12182870-Enzyme Inhibitors,
pubmed-meshheading:12182870-Humans,
pubmed-meshheading:12182870-Lipoproteins,
pubmed-meshheading:12182870-Phospholipases A,
pubmed-meshheading:12182870-Pyrimidinones,
pubmed-meshheading:12182870-Rabbits,
pubmed-meshheading:12182870-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.
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pubmed:affiliation |
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, SG1 2NY, Stevenage, UK.
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pubmed:publicationType |
Journal Article
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