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Design, synthesis and 5-HT/NE dual reuptake inhibitory activity of aromatic heterocyclic arylamidine derivatives / 药学学报
Acta Pharmaceutica Sinica ; (12): 303-308, 2009.
Article Dans Chinois | WPRIM | ID: wpr-278266
ABSTRACT
Based on the pharmacophore information and the analysis of structure-activity relationship of SSRIs and SNRIs, a series of substituted aromatic heterocyclic arylamidine derivatives were designed and synthesized in order to search for lead compounds with dual activity. All of them were new compounds, and their structures were confirmed by 1H NMR and HRMS. Preliminary in vitro pharmacological tests showed that all target compounds exhibited 5-HT reuptake inhibitory activity and some compounds exhibited NE reuptake inhibitory activity. These aromatic heterocyclic arylamidine designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Sujets)
Texte intégral: Disponible Indice: WPRIM (Pacifique occidental) Sujet Principal: Pharmacologie / Relation structure-activité / Synapses / Conception de médicament / Sérotonine / Norépinéphrine / Chimie / Inbiteurs sélectifs de la recapture de la sérotonine / Rat Wistar / Inhibiteurs de la capture des neurotransmetteurs Type d'étude: Étude pronostique Limites du sujet: Animaux langue: Chinois Texte intégral: Acta Pharmaceutica Sinica Année: 2009 Type: Article

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Texte intégral: Disponible Indice: WPRIM (Pacifique occidental) Sujet Principal: Pharmacologie / Relation structure-activité / Synapses / Conception de médicament / Sérotonine / Norépinéphrine / Chimie / Inbiteurs sélectifs de la recapture de la sérotonine / Rat Wistar / Inhibiteurs de la capture des neurotransmetteurs Type d'étude: Étude pronostique Limites du sujet: Animaux langue: Chinois Texte intégral: Acta Pharmaceutica Sinica Année: 2009 Type: Article