New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with α2-Adrenoceptor antagonist activity
Identifieur interne : 003B68 ( Main/Curation ); précédent : 003B67; suivant : 003B69New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with α2-Adrenoceptor antagonist activity
Auteurs : Patrice Mayer [France] ; Pascale Brunel [France] ; Céline Chaplain [France] ; Christel Piedecoq [France] ; Francis Calmel [France] ; Philippe Schambel [France] ; Philippe Chopin [France] ; Thierry Wurch [France] ; Petrus J. Pauwels [France] ; Marc Marien [France] ; Jean-Louis Vidaluc [France] ; Thierry Imbert [France]Source :
- Journal of medicinal chemistry : (Print) [ 0022-2623 ] ; 2000.
Descripteurs français
- Pascal (Inist)
- Relation structure activité, Antagoniste, Récepteur α2-adrénergique, Sélectivité, In vitro, In vivo, Animal, Souris, Durée action, Longue durée, Pharmacocinétique, Biodisponibilité, Synthèse chimique, Imidazole dérivé, Hétérocycle azote, Urées, Pipéridine dérivé, Hétérocycle oxygène, Composé bicyclique, Composé aromatique, 1,4-Benzodioxine dérivé, Imidazolidin-2-one(1-[2-(1-[2,3-dihydro-1,4-benzodioxin-2-ylméthyl]-4-pipéridyl)éthyl]-3-[2,4,6-triméthoxyphényl]).
English descriptors
- KwdEn :
- Animal, Antagonist, Aromatic compound, Bicyclic compound, Bioavailability, Chemical synthesis, Duration of action, Imidazole derivatives, In vitro, In vivo, Long lasting, Mouse, Nitrogen heterocycle, Oxygen heterocycle, Pharmacokinetics, Piperidine derivatives, Selectivity, Structure activity relation, Ureas, α2-Adrenergic receptor.
Abstract
The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α2-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent α2-adrenoceptor antagonists with good selectivity versus α1-adrenergic and D2-dopamine receptors. Particular emphasis is given to compound 33g which displays potent α2-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.
Links toward previous steps (curation, corpus...)
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Links to Exploration step
Pascal:00-0514031Le document en format XML
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-Adrenoceptor antagonist activity</title>
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<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a">New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with α<sub>2</sub>
-Adrenoceptor antagonist activity</title>
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<author><name sortKey="Pauwels, Petrus J" sort="Pauwels, Petrus J" uniqKey="Pauwels P" first="Petrus J." last="Pauwels">Petrus J. Pauwels</name>
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<author><name sortKey="Vidaluc, Jean Louis" sort="Vidaluc, Jean Louis" uniqKey="Vidaluc J" first="Jean-Louis" last="Vidaluc">Jean-Louis Vidaluc</name>
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<author><name sortKey="Imbert, Thierry" sort="Imbert, Thierry" uniqKey="Imbert T" first="Thierry" last="Imbert">Thierry Imbert</name>
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<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>11 aut.</sZ>
<sZ>12 aut.</sZ>
</inist:fA14>
<country>France</country>
<placeName><region type="region" nuts="2">Occitanie (région administrative)</region>
<region type="old region" nuts="2">Midi-Pyrénées</region>
<settlement type="city">Castres</settlement>
</placeName>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">Journal of medicinal chemistry : (Print)</title>
<title level="j" type="abbreviated">J. med. chem. : (Print)</title>
<idno type="ISSN">0022-2623</idno>
<imprint><date when="2000">2000</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><title level="j" type="main">Journal of medicinal chemistry : (Print)</title>
<title level="j" type="abbreviated">J. med. chem. : (Print)</title>
<idno type="ISSN">0022-2623</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animal</term>
<term>Antagonist</term>
<term>Aromatic compound</term>
<term>Bicyclic compound</term>
<term>Bioavailability</term>
<term>Chemical synthesis</term>
<term>Duration of action</term>
<term>Imidazole derivatives</term>
<term>In vitro</term>
<term>In vivo</term>
<term>Long lasting</term>
<term>Mouse</term>
<term>Nitrogen heterocycle</term>
<term>Oxygen heterocycle</term>
<term>Pharmacokinetics</term>
<term>Piperidine derivatives</term>
<term>Selectivity</term>
<term>Structure activity relation</term>
<term>Ureas</term>
<term>α2-Adrenergic receptor</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Relation structure activité</term>
<term>Antagoniste</term>
<term>Récepteur α2-adrénergique</term>
<term>Sélectivité</term>
<term>In vitro</term>
<term>In vivo</term>
<term>Animal</term>
<term>Souris</term>
<term>Durée action</term>
<term>Longue durée</term>
<term>Pharmacocinétique</term>
<term>Biodisponibilité</term>
<term>Synthèse chimique</term>
<term>Imidazole dérivé</term>
<term>Hétérocycle azote</term>
<term>Urées</term>
<term>Pipéridine dérivé</term>
<term>Hétérocycle oxygène</term>
<term>Composé bicyclique</term>
<term>Composé aromatique</term>
<term>1,4-Benzodioxine dérivé</term>
<term>Imidazolidin-2-one(1-[2-(1-[2,3-dihydro-1,4-benzodioxin-2-ylméthyl]-4-pipéridyl)éthyl]-3-[2,4,6-triméthoxyphényl])</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">The emergence of a novel theory concerning the role of noradrenaline in the progression and the treatment of neurodegenerative diseases such as Parkinson's and Alzheimer's diseases has provided a new impetus toward the discovery of novel compounds acting at α<sub>2</sub>
-adrenoceptors. A series of substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives bearing an amide, urea, or imidazolidinone moiety was studied. Some members of this series of compounds proved to be potent α<sub>2</sub>
-adrenoceptor antagonists with good selectivity versus α<sub>1</sub>
-adrenergic and D<sub>2</sub>
-dopamine receptors. Particular emphasis is given to compound 33g which displays potent α<sub>2</sub>
-adrenoceptor binding affinity in vitro and central effects in vivo following oral administration.</div>
</front>
</TEI>
</record>
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