Source:http://linkedlifedata.com/resource/pubmed/id/20346666
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2010-4-5
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pubmed:abstractText |
We previously reported a novel pyrrole derivative 1 which possesses a tetrahydropyridine group at the beta-position with a proinflammatory cytokine TNFalpha production inhibitor. Herein, we report the synthesis and biological activity of N- and alpha-position substituted tetrahydropyridine derivatives. In this series, we found that compound 3o showed good inhibitory activity in vitro (inhibition of lipopolysaccharide (LPS)-induced TNFalpha production in human whole blood, IC(50)=0.44 microM) and compound 3i demonstrated potent inhibitory activity in vivo (inhibition of LPS-induced TNFalpha production in mice, ID(50)=1.42 mg/kg).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:copyrightInfo |
Crown Copyright 2010. Published by Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2435-7
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pubmed:meshHeading |
pubmed-meshheading:20346666-Animals,
pubmed-meshheading:20346666-Humans,
pubmed-meshheading:20346666-Inflammation Mediators,
pubmed-meshheading:20346666-Lipopolysaccharides,
pubmed-meshheading:20346666-Mice,
pubmed-meshheading:20346666-Pyridines,
pubmed-meshheading:20346666-Tumor Necrosis Factor-alpha
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pubmed:year |
2010
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pubmed:articleTitle |
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.
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pubmed:affiliation |
Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd, Edogawa-ku, Tokyo134-8630, Japan. nakao.akira.g5@daiichisankyo.co.jp
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pubmed:publicationType |
Journal Article
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