Source:http://linkedlifedata.com/resource/pubmed/id/21421310
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2011-4-4
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pubmed:abstractText |
Pathological calcifications induced by deposition of basic phosphate crystals or hydroxyapatite (HA) on soft tissues are a large family of diseases comprising of ankylosing spondylitis (AS), end-stage osteoarthritis (OA) and vascular calcification. High activity of tissue non-specific alkaline phosphatase (TNAP) is a hallmark of pathological calcifications induced by HA deposition. The use of TNAP inhibitor is a possible therapeutic option to address calcific diseases produced by HA deposition on soft tissues. We report the synthesis of a series of thiopheno-imidazo[2,1-b]thiazole derivatives which were evaluated as potential inhibitors of TNAP displaying a large range of IC(50) at pH 10.4 (from 42±13 ?M to more than 800 ?M).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Alkaline Phosphatase,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Phenols,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfhydryl Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/thiophenol
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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 |
Copyright © 2011. Published by Elsevier Ltd.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2297-301
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pubmed:meshHeading |
pubmed-meshheading:21421310-Alkaline Phosphatase,
pubmed-meshheading:21421310-Calcinosis,
pubmed-meshheading:21421310-Enzyme Inhibitors,
pubmed-meshheading:21421310-Humans,
pubmed-meshheading:21421310-Hydrogen-Ion Concentration,
pubmed-meshheading:21421310-Phenols,
pubmed-meshheading:21421310-Sulfhydryl Compounds,
pubmed-meshheading:21421310-Thiazoles
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pubmed:year |
2011
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pubmed:articleTitle |
Synthesis and evaluation of thiophenyl derivatives as inhibitors of alkaline phosphatase.
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pubmed:affiliation |
Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, UMR-CNRS 5246, Equipe Catalyse Synthèse Environnement, Université Claude Bernard-Lyon 1, Bâtiment Curien, 43 Bd du 11 Novembre 1918, F-69622 Villeurbanne, France.
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pubmed:publicationType |
Journal Article
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