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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 |
2004-12-17
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pubmed:abstractText |
Replacement of the morpholinyl moiety in (S,E)-N-[1-(3-morpholinophenyl)ethyl]-3-phenylacrylamide (1) with heteroaryl groups led to the identification of (S,E)-N-1-[3-(6-fluoropyridin-3-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (5) as a potent KCNQ2 potassium channel opener. Among this series of heteroaryl substituted acrylamides, (S,E)-N-1-[3-(1H-pyrazol-1-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (9) exhibits balanced potency and efficacy. The syntheses and the KCNQ2 opener activity of this series of acrylamides are described.
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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:ChenJieJ,
pubmed-author:DworetzkySteven ISI,
pubmed-author:HardenDavid GDG,
pubmed-author:HeHuanH,
pubmed-author:KnoxRonald JRJ,
pubmed-author:L'HeureuxAlexandreA,
pubmed-author:MartelAlainA,
pubmed-author:NataleJoanneJ,
pubmed-author:StarrettJohn EJE,
pubmed-author:SunLi-QiangLQ,
pubmed-author:ThompsonMark WMW,
pubmed-author:WeaverDavidD,
pubmed-author:WuYong-JinYJ
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pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
363-6
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:15603955-Acrylamides,
pubmed-meshheading:15603955-Action Potentials,
pubmed-meshheading:15603955-Animals,
pubmed-meshheading:15603955-Cell Line,
pubmed-meshheading:15603955-Dose-Response Relationship, Drug,
pubmed-meshheading:15603955-Humans,
pubmed-meshheading:15603955-KCNQ2 Potassium Channel,
pubmed-meshheading:15603955-Molecular Structure,
pubmed-meshheading:15603955-Potassium Channels, Voltage-Gated
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pubmed:year |
2005
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pubmed:articleTitle |
(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.
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pubmed:affiliation |
Department of Medicinal Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 100 de l'Industrie Blvd., Candiac, Quebec, Canada, J5R 1J1.
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pubmed:publicationType |
Journal Article
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