title: [Design, synthesis and 5-HT/NE dual reuptake inhibitory activity of aromatic heterocyclic arylamidine derivatives].
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.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Wen
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.forename: Jian-jun
authors.initials: JJ
authors.lastname: Zhang
authors.forename: Ya-fang
authors.initials: YF
authors.lastname: Wang
authors.forename: Cheng-xue
authors.initials: CX
authors.lastname: Ji
authors.forename: Guang-zhong
authors.initials: GZ
authors.lastname: Yang
mesh_terms: D000578:Amidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D009638:Norepinephrine / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D012701:Serotonin / Q000378:metabolism*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013569:Synapses / Q000378:metabolism
chemical_list: D000578:Amidines; D000928:Antidepressive Agents; D006571:Heterocyclic Compounds; D014179:Neurotransmitter Uptake Inhibitors; D009638:Norepinephrine; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors