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rdf:type |
|
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lifeskim:mentions |
umls-concept:C0205177,
umls-concept:C0205314,
umls-concept:C0205531,
umls-concept:C0205549,
umls-concept:C0226896,
umls-concept:C0243076,
umls-concept:C0442027,
umls-concept:C0679622,
umls-concept:C1424685,
umls-concept:C1527415,
umls-concept:C1880355
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|
pubmed:issue |
14
|
|
pubmed:dateCreated |
2008-7-21
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|
pubmed:abstractText |
Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious gamma-lactam series of selective NK(1) antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.
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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 |
|
|
pubmed:status |
MEDLINE
|
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pubmed:month |
Jul
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|
pubmed:issn |
1464-3405
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|
pubmed:author |
pubmed-author:DuffyRuth ARA,
pubmed-author:LachowiczJean EJE,
pubmed-author:NomeirAmin AAA,
pubmed-author:PaliwalSunilS,
pubmed-author:ReichardGregory AGA,
pubmed-author:ShahSapnaS,
pubmed-author:ShihNeng-YangNY,
pubmed-author:StengoneCarmineC,
pubmed-author:TsuiHon-ChungHC,
pubmed-author:VartyGeoffrey BGB,
pubmed-author:WangChengC,
pubmed-author:WrobleskiMichelle LaciML,
pubmed-author:XiaoDongD
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|
pubmed:issnType |
Electronic
|
|
pubmed:day |
15
|
|
pubmed:volume |
18
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
4168-71
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|
pubmed:meshHeading |
pubmed-meshheading:18547807-Administration, Oral,
pubmed-meshheading:18547807-Chemistry, Pharmaceutical,
pubmed-meshheading:18547807-Drug Design,
pubmed-meshheading:18547807-Humans,
pubmed-meshheading:18547807-Lactams,
pubmed-meshheading:18547807-Models, Chemical,
pubmed-meshheading:18547807-Molecular Structure,
pubmed-meshheading:18547807-Nitrogen,
pubmed-meshheading:18547807-Protein Binding,
pubmed-meshheading:18547807-Receptors, Neurokinin-1,
pubmed-meshheading:18547807-Structure-Activity Relationship,
pubmed-meshheading:18547807-Substance P,
pubmed-meshheading:18547807-Urea,
pubmed-meshheading:18547807-Vomiting
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
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|
pubmed:affiliation |
Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. sunil.paliwal@spcorp.com
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pubmed:publicationType |
Journal Article
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