Design, synthesis and pharmacological investigation of isoindoline derivatives as 5-HT/NE double reuptake inhibitors.
- Author:
Hui WEN
;
Yuan SHI
;
Jing-wen DONG
;
Yan-shen GUO
;
Jian-Jun ZANG
;
Guang-zhong YANG
- Publication Type:Journal Article
- MeSH:
Antidepressive Agents;
chemical synthesis;
chemistry;
Biological Transport;
Drug Design;
Isoindoles;
chemical synthesis;
chemistry;
Serotonin Uptake Inhibitors;
chemical synthesis;
chemistry;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2015;50(9):1148-1155
- CountryChina
- Language:Chinese
-
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.
