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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2001-2-5
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pubmed:abstractText |
Described are the acylation binding of trans-lactam 1 to porcine pancreatic elastase, the selection of the SO2Me activating group for the lactam N which also confers metabolic stability in hamster liver microsomes, the introduction of aqueous solubility through the piperidine salt 9, the in vivo oral activity of 9 and its bioavailability, and the introduction of 9 as an intracellular neutrophil elastase inhibitor.
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pubmed:commentsCorrections |
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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 |
0960-894X
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pubmed:author |
pubmed-author:BeltonD JDJ,
pubmed-author:ClarkeG DGD,
pubmed-author:DixonMM,
pubmed-author:DowleM DMD,
pubmed-author:FinchHH,
pubmed-author:FleetwoodGG,
pubmed-author:GodwardR ERE,
pubmed-author:HardyG WGW,
pubmed-author:HarrisonL ALA,
pubmed-author:HodgsonS TST,
pubmed-author:HumphreysD CDC,
pubmed-author:InglisG GGG,
pubmed-author:JohnsonM RMR,
pubmed-author:KumarK AKA,
pubmed-author:MacdonaldS JSJ,
pubmed-author:McDonaldEE,
pubmed-author:MolloyC RCR,
pubmed-author:MurkittGG,
pubmed-author:ShahPP,
pubmed-author:SinghO MOM,
pubmed-author:SkarzynskiTT,
pubmed-author:SmithR ARA,
pubmed-author:SpoonerJ EJE
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
243-6
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:11206469-Acylation,
pubmed-meshheading:11206469-Administration, Oral,
pubmed-meshheading:11206469-Animals,
pubmed-meshheading:11206469-Binding Sites,
pubmed-meshheading:11206469-Cricetinae,
pubmed-meshheading:11206469-Crystallography, X-Ray,
pubmed-meshheading:11206469-Enzyme Inhibitors,
pubmed-meshheading:11206469-Humans,
pubmed-meshheading:11206469-Inhibitory Concentration 50,
pubmed-meshheading:11206469-Lactams,
pubmed-meshheading:11206469-Leukocyte Elastase,
pubmed-meshheading:11206469-Models, Molecular,
pubmed-meshheading:11206469-Neutrophils,
pubmed-meshheading:11206469-Pancreas,
pubmed-meshheading:11206469-Protein Binding,
pubmed-meshheading:11206469-Pyrrolidines,
pubmed-meshheading:11206469-Solubility,
pubmed-meshheading:11206469-Structure-Activity Relationship,
pubmed-meshheading:11206469-Swine
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pubmed:year |
2001
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pubmed:articleTitle |
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
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pubmed:affiliation |
Medical Chemistry 2, Glaxo Wellcome Medicines Research Centre, Stevenage, UK. sjfm5947@glaxowellcome.co.uk
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pubmed:publicationType |
Journal Article
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