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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
2010-4-5
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).
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
1464-3405
pubmed:author
pubmed:copyrightInfo
Crown Copyright 2010. Published by Elsevier Ltd. All rights reserved.
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
20
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2435-7
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.
pubmed:affiliation
Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd, Edogawa-ku, Tokyo134-8630, Japan. nakao.akira.g5@daiichisankyo.co.jp
pubmed:publicationType
Journal Article