Source:http://linkedlifedata.com/resource/pubmed/id/20188553
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
7
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| pubmed:dateCreated |
2010-3-22
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| pubmed:abstractText |
A new class of potent NK(1) receptor antagonists with a tetrahydroindolizinone core has been identified. This series of compounds demonstrated improved functional activities as compared to previously identified 5,5-fused pyrrolidine lead structures. SAR at the 7-position of the tetrahydroindolizinone core is discussed in detail. A number of compounds displayed high NK(1) receptor occupancy at both 1 h and 24 h in a gerbil foot tapping model. Compound 40 has high NK(1) binding affinity, good selectivity for other NK receptors and promising in vivo properties. It also has clean P(450) inhibition and hPXR induction profiles.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Apr
|
| pubmed:issn |
1464-3405
|
| pubmed:author |
pubmed-author:BaoJianmingJ,
pubmed-author:CarlsonEmma JEJ,
pubmed-author:ChicchiGary GGG,
pubmed-author:DeVitaRobert JRJ,
pubmed-author:KurtzMarc MMM,
pubmed-author:LuHuagangH,
pubmed-author:MillsSander GSG,
pubmed-author:MorrielloGregori JGJ,
pubmed-author:TongXinchunX,
pubmed-author:TsaoKwei-Lan CKL,
pubmed-author:WheeldonAlanA,
pubmed-author:ZhengSongS
|
| pubmed:copyrightInfo |
2010 Elsevier Ltd. All rights reserved.
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| pubmed:issnType |
Electronic
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| pubmed:day |
1
|
| pubmed:volume |
20
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
2354-8
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| pubmed:meshHeading | |
| pubmed:year |
2010
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| pubmed:articleTitle |
Tetrahydroindolizinone NK1 antagonists.
|
| pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. bao_jianming@merck.com
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| pubmed:publicationType |
Journal Article
|