title: [Design, synthesis and pharmacological investigation of isoindoline derivatives as 5-HT/NE double reuptake inhibitors].
abstract: A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
authors.forename: Hui
authors.initials: H
authors.lastname: Wen
authors.forename: Yuan
authors.initials: Y
authors.lastname: Shi
authors.forename: Jing-wen
authors.initials: JW
authors.lastname: Dong
authors.forename: Yan-shen
authors.initials: YS
authors.lastname: Guo
authors.forename: Jian-Jun
authors.initials: JJ
authors.lastname: Zang
authors.forename: Guang-zhong
authors.initials: GZ
authors.lastname: Yang
mesh_terms: D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry*; D001692:Biological Transport; D015195:Drug Design; D054833:Isoindoles / Q000138:chemical synthesis / Q000737:chemistry*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000928:Antidepressive Agents; D054833:Isoindoles; D017367:Selective Serotonin Reuptake Inhibitors