Source:http://linkedlifedata.com/resource/pubmed/id/21139262
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2010-12-8
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pubmed:abstractText |
We have previously disclosed that some 6,7-dimethoxyisoquinoline derivatives are able to produce anticonvulsant effects in different animal models of epilepsy. Following these studies this paper describes the synthesis of a small series of new 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines strictly related to previously reported analogues. This novel series of isoquinolines was designed on the basis of well defined structure-active relationship (SAR) information already acquired for this class of anticonvulsant agents. The pharmacological effects of the new synthesized compounds were evaluated against audiogenic seizures in Dilute Brown non-Agouti (DBA/2) mice. The preliminary pharmacological screening led to the identification of a new active molecule the 2-acetyl-1-(4'-methylphenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (6d) that displayed significant anticonvulsant activity. Computational studies helped to rationalize these obtained pharmacological results.
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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:issn |
1347-5223
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
58
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1602-5
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pubmed:meshHeading |
pubmed-meshheading:21139262-Animals,
pubmed-meshheading:21139262-Anticonvulsants,
pubmed-meshheading:21139262-Mice,
pubmed-meshheading:21139262-Mice, Inbred DBA,
pubmed-meshheading:21139262-Models, Molecular,
pubmed-meshheading:21139262-Seizures,
pubmed-meshheading:21139262-Structure-Activity Relationship,
pubmed-meshheading:21139262-Tetrahydroisoquinolines
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and structure-active relationship of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline anticonvulsants.
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pubmed:affiliation |
Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. rgitto@unime.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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