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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2006-1-9
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pubmed:abstractText |
A series of novel five-membered urea derivatives as potent NK1 receptor antagonists is described. The effects of substitution of a 4-fluoro group at the phenyl ring and the introduction of an alpha-methyl group at the benzylic position to improve potency and duration of in vivo activity are discussed. Several compounds with high affinity and sustained in vivo activity were identified.
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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 |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BlythinDavid JDJ,
pubmed-author:ChenXiaoX,
pubmed-author:CoffinVicki LVL,
pubmed-author:DuffyRuth ARA,
pubmed-author:GuDanlinD,
pubmed-author:LachowiczJean EJE,
pubmed-author:LinLingL,
pubmed-author:MorganCynthia ACA,
pubmed-author:NomeirAmin AAA,
pubmed-author:PaliwalSunilS,
pubmed-author:PiwinskiJohn JJJ,
pubmed-author:ReichardGregory AGA,
pubmed-author:SchwerdtJohn HJH,
pubmed-author:ShihNeng-YangNY,
pubmed-author:ShueHo-JaneHJ,
pubmed-author:VartyGeoffrey BGB,
pubmed-author:WangChengC,
pubmed-author:WangHongwuH
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1065-9
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pubmed:meshHeading |
pubmed-meshheading:16290143-Animals,
pubmed-meshheading:16290143-Anti-Anxiety Agents,
pubmed-meshheading:16290143-Benzyl Alcohols,
pubmed-meshheading:16290143-Crystallography, X-Ray,
pubmed-meshheading:16290143-Drug Evaluation, Preclinical,
pubmed-meshheading:16290143-Fluorine,
pubmed-meshheading:16290143-Gerbillinae,
pubmed-meshheading:16290143-Models, Molecular,
pubmed-meshheading:16290143-Molecular Structure,
pubmed-meshheading:16290143-Motor Activity,
pubmed-meshheading:16290143-Receptors, Neurokinin-1,
pubmed-meshheading:16290143-Structure-Activity Relationship,
pubmed-meshheading:16290143-Urea
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pubmed:year |
2006
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pubmed:articleTitle |
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
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pubmed:affiliation |
Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
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pubmed:publicationType |
Journal Article
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