Design, synthesis and pharmacological investigation of isoindoline derivatives as 5-HT/NE double reuptake inhibitors.
- Author:
Hui WEN
;
Yuan SHI
;
Jingwen DONG
;
Yanshen GUO
;
Jianjun ZANG
;
Guangzhong YANG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2015;50(9):1148-55
- 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.
