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rdf:type |
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lifeskim:mentions |
umls-concept:C0050587,
umls-concept:C0205314,
umls-concept:C0205360,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243072,
umls-concept:C0243076,
umls-concept:C0311400,
umls-concept:C0679622,
umls-concept:C1413189,
umls-concept:C1883254
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pubmed:issue |
16
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pubmed:dateCreated |
2009-8-11
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|
pubmed:abstractText |
Our laboratory has identified several acrylamide derivatives with potent CCR3 inhibitory activity. In the present study, we evaluated the in vitro metabolic stability (CL(int); mL/min/kg) of these compounds in human liver microsomes (HLMs), and assessed the relationship between their structures and CL(int) values. Among the compounds identified, N-{(3R)-1-[(6-fluoro-2-naphthyl)methyl]pyrrolidin-3-yl}-2-[1-(2-hydroxybenzoyl)piperidin-4-ylidene]acetamide (30j) was found to be a potent inhibitor (IC(50)=8.4nM) with a high metabolic stability against HLMs.
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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 |
Aug
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:ImaokaTakayukiT,
pubmed-author:InamiHiroshiH,
pubmed-author:IuraYosukeY,
pubmed-author:KubotaHirokazuH,
pubmed-author:MorihiraKoichiroK,
pubmed-author:MorokataTatsuakiT,
pubmed-author:NittaAikoA,
pubmed-author:OhnoKazukiK,
pubmed-author:OhtaMitsuakiM,
pubmed-author:SatoIppeiI,
pubmed-author:SuzukiKeikoK,
pubmed-author:TakahashiToshiyaT,
pubmed-author:TakeuchiMakotoM,
pubmed-author:TsukamotoShin-ichiS
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pubmed:issnType |
Electronic
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pubmed:day |
15
|
|
pubmed:volume |
17
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
5989-6002
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pubmed:meshHeading |
pubmed-meshheading:19620010-Acetamides,
pubmed-meshheading:19620010-Acrylamides,
pubmed-meshheading:19620010-Animals,
pubmed-meshheading:19620010-Anti-Allergic Agents,
pubmed-meshheading:19620010-Haplorhini,
pubmed-meshheading:19620010-Humans,
pubmed-meshheading:19620010-Mice,
pubmed-meshheading:19620010-Microsomes, Liver,
pubmed-meshheading:19620010-Naphthalenes,
pubmed-meshheading:19620010-Piperidines,
pubmed-meshheading:19620010-Protein Isoforms,
pubmed-meshheading:19620010-Receptors, CCR3,
pubmed-meshheading:19620010-Thermodynamics
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis, biological evaluation, and metabolic stability of acrylamide derivatives as novel CCR3 antagonists.
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pubmed:affiliation |
Astellas Pharma Inc., Miyukigaoka, Tsukuba-shi, Ibaraki, Japan. ippei.sato@jp.astellas.com
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pubmed:publicationType |
Journal Article
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