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...)
- to stream PascalFrancis, to step Corpus: Pour aller vers cette notice dans l'étape Curation :001301
- to stream PascalFrancis, to step Curation: Pour aller vers cette notice dans l'étape Curation :000137
- to stream PascalFrancis, to step Checkpoint: Pour aller vers cette notice dans l'étape Curation :001190
- to stream Main, to step Merge: Pour aller vers cette notice dans l'étape Curation :004227
Links to Exploration step
Pascal:00-0514031Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><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><author><name sortKey="Mayer, Patrice" sort="Mayer, Patrice" uniqKey="Mayer P" first="Patrice" last="Mayer">Patrice Mayer</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Brunel, Pascale" sort="Brunel, Pascale" uniqKey="Brunel P" first="Pascale" last="Brunel">Pascale Brunel</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Chaplain, Celine" sort="Chaplain, Celine" uniqKey="Chaplain C" first="Céline" last="Chaplain">Céline Chaplain</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Piedecoq, Christel" sort="Piedecoq, Christel" uniqKey="Piedecoq C" first="Christel" last="Piedecoq">Christel Piedecoq</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Calmel, Francis" sort="Calmel, Francis" uniqKey="Calmel F" first="Francis" last="Calmel">Francis Calmel</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Schambel, Philippe" sort="Schambel, Philippe" uniqKey="Schambel P" first="Philippe" last="Schambel">Philippe Schambel</name><affiliation wicri:level="3"><inist:fA14 i1="02"><s1>Department of Analytical Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>6 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><author><name sortKey="Chopin, Philippe" sort="Chopin, Philippe" uniqKey="Chopin P" first="Philippe" last="Chopin">Philippe Chopin</name><affiliation wicri:level="3"><inist:fA14 i1="03"><s1>Division of Neurobiology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>7 aut.</sZ><sZ>10 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><author><name sortKey="Wurch, Thierry" sort="Wurch, Thierry" uniqKey="Wurch T" first="Thierry" last="Wurch">Thierry Wurch</name><affiliation wicri:level="3"><inist:fA14 i1="04"><s1>Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>8 aut.</sZ><sZ>9 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><author><name sortKey="Pauwels, Petrus J" sort="Pauwels, Petrus J" uniqKey="Pauwels P" first="Petrus J." last="Pauwels">Petrus J. Pauwels</name><affiliation wicri:level="3"><inist:fA14 i1="04"><s1>Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>8 aut.</sZ><sZ>9 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><author><name sortKey="Marien, Marc" sort="Marien, Marc" uniqKey="Marien M" first="Marc" last="Marien">Marc Marien</name><affiliation wicri:level="3"><inist:fA14 i1="03"><s1>Division of Neurobiology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>7 aut.</sZ><sZ>10 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><author><name sortKey="Vidaluc, Jean Louis" sort="Vidaluc, Jean Louis" uniqKey="Vidaluc J" first="Jean-Louis" last="Vidaluc">Jean-Louis Vidaluc</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Imbert, Thierry" sort="Imbert, Thierry" uniqKey="Imbert T" first="Thierry" last="Imbert">Thierry Imbert</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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></titleStmt><publicationStmt><idno type="wicri:source">INIST</idno><idno type="inist">00-0514031</idno><date when="2000">2000</date><idno type="stanalyst">PASCAL 00-0514031 INIST</idno><idno type="RBID">Pascal:00-0514031</idno><idno type="wicri:Area/PascalFrancis/Corpus">001301</idno><idno type="wicri:Area/PascalFrancis/Curation">000137</idno><idno type="wicri:Area/PascalFrancis/Checkpoint">001190</idno><idno type="wicri:explorRef" wicri:stream="PascalFrancis" wicri:step="Checkpoint">001190</idno><idno type="wicri:doubleKey">0022-2623:2000:Mayer P:new:substituted:dihydrobenzo</idno><idno type="wicri:Area/Main/Merge">004227</idno><idno type="wicri:Area/Main/Curation">003B68</idno></publicationStmt><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><author><name sortKey="Mayer, Patrice" sort="Mayer, Patrice" uniqKey="Mayer P" first="Patrice" last="Mayer">Patrice Mayer</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Brunel, Pascale" sort="Brunel, Pascale" uniqKey="Brunel P" first="Pascale" last="Brunel">Pascale Brunel</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Chaplain, Celine" sort="Chaplain, Celine" uniqKey="Chaplain C" first="Céline" last="Chaplain">Céline Chaplain</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Piedecoq, Christel" sort="Piedecoq, Christel" uniqKey="Piedecoq C" first="Christel" last="Piedecoq">Christel Piedecoq</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Calmel, Francis" sort="Calmel, Francis" uniqKey="Calmel F" first="Francis" last="Calmel">Francis Calmel</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Schambel, Philippe" sort="Schambel, Philippe" uniqKey="Schambel P" first="Philippe" last="Schambel">Philippe Schambel</name><affiliation wicri:level="3"><inist:fA14 i1="02"><s1>Department of Analytical Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>6 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><author><name sortKey="Chopin, Philippe" sort="Chopin, Philippe" uniqKey="Chopin P" first="Philippe" last="Chopin">Philippe Chopin</name><affiliation wicri:level="3"><inist:fA14 i1="03"><s1>Division of Neurobiology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>7 aut.</sZ><sZ>10 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><author><name sortKey="Wurch, Thierry" sort="Wurch, Thierry" uniqKey="Wurch T" first="Thierry" last="Wurch">Thierry Wurch</name><affiliation wicri:level="3"><inist:fA14 i1="04"><s1>Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>8 aut.</sZ><sZ>9 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><author><name sortKey="Pauwels, Petrus J" sort="Pauwels, Petrus J" uniqKey="Pauwels P" first="Petrus J." last="Pauwels">Petrus J. Pauwels</name><affiliation wicri:level="3"><inist:fA14 i1="04"><s1>Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>8 aut.</sZ><sZ>9 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><author><name sortKey="Marien, Marc" sort="Marien, Marc" uniqKey="Marien M" first="Marc" last="Marien">Marc Marien</name><affiliation wicri:level="3"><inist:fA14 i1="03"><s1>Division of Neurobiology, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>7 aut.</sZ><sZ>10 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><author><name sortKey="Vidaluc, Jean Louis" sort="Vidaluc, Jean Louis" uniqKey="Vidaluc J" first="Jean-Louis" last="Vidaluc">Jean-Louis Vidaluc</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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><author><name sortKey="Imbert, Thierry" sort="Imbert, Thierry" uniqKey="Imbert T" first="Thierry" last="Imbert">Thierry Imbert</name><affiliation wicri:level="3"><inist:fA14 i1="01"><s1>Division of Medicinal Chemistry, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin</s1><s2>81100 Castres</s2><s3>FRA</s3><sZ>1 aut.</sZ><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>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Wicri/Sante/explor/ParkinsonFranceV1/Data/Main/Curation
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 003B68 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Curation/biblio.hfd -nk 003B68 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Wicri/Sante
|area= ParkinsonFranceV1
|flux= Main
|étape= Curation
|type= RBID
|clé= Pascal:00-0514031
|texte= New substituted 1-(2,3-dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl derivatives with α2-Adrenoceptor antagonist activity
}}
| This area was generated with Dilib version V0.6.29. |  |