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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2005-6-1
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pubmed:abstractText |
Five new piperidine alkaloids were designed from natural (-)-3-O-acetyl-spectaline and (-)-spectaline that were obtained from the flowers of Senna spectabilis (sin. Cassia spectabilis, Leguminosae). Two semi-synthetic analogues (7 and 9) inhibited rat brain acetylcholinesterase, showing IC50 of 7.32 and 15.1 microM, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1mg/kg, i.p.) was fully efficacious in reverting scopolamine-induced amnesia in mice. The two active compounds (7 and 9) did not show overt toxic effects at the doses tested in vivo.
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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 |
Jul
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pubmed:issn |
0968-0896
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pubmed:author |
pubmed-author:BarreiroEliezer JEJ,
pubmed-author:BolzaniVanderlan SVS,
pubmed-author:CabralRafael FRF,
pubmed-author:CastroNewton GNG,
pubmed-author:CostaRodrigo SRS,
pubmed-author:FloydCorinneC,
pubmed-author:FragaCarlos A MCA,
pubmed-author:PimentelLuísa S BLS,
pubmed-author:RochaMônica SMS,
pubmed-author:ViegasCláudioCJr,
pubmed-author:YoungMaria C MMC
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4184-90
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:15878668-Acetylcholinesterase,
pubmed-meshheading:15878668-Alkaloids,
pubmed-meshheading:15878668-Amnesia,
pubmed-meshheading:15878668-Animals,
pubmed-meshheading:15878668-Brain,
pubmed-meshheading:15878668-Butyrylcholinesterase,
pubmed-meshheading:15878668-Cholinesterase Inhibitors,
pubmed-meshheading:15878668-Drug Design,
pubmed-meshheading:15878668-Flowers,
pubmed-meshheading:15878668-Male,
pubmed-meshheading:15878668-Mice,
pubmed-meshheading:15878668-Molecular Structure,
pubmed-meshheading:15878668-Muscarinic Antagonists,
pubmed-meshheading:15878668-Piperidines,
pubmed-meshheading:15878668-Plant Extracts,
pubmed-meshheading:15878668-Plants, Medicinal,
pubmed-meshheading:15878668-Rats,
pubmed-meshheading:15878668-Rats, Wistar,
pubmed-meshheading:15878668-Scopolamine Hydrobromide,
pubmed-meshheading:15878668-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids.
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pubmed:affiliation |
Laboratório de Avaliação e Síntese, de Substâncias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, CP 68023, 21944-910, Rio de Janeiro, Brazil.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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