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Synthesis and 5-HT reuptake inhibition activity of biarylbenzamidine derivatives

Qin, F.; Wang, N-Sha.; Yang, J.; Zhang, J-Jun.; Wang, Y-Fang.; Yang, G-Zhong.

Yao Xue Xue Bao 43(6): 619-625

2008

ISSN/ISBN: 0513-4870
PMID: 18822965
Document Number: 627621
A series of biarylbenzamidine analogs were synthesized and tested for their biological activities of inhibiting the reuptake of 5-HT. All of them were new compounds, and their structures were confirmed by H-1 NMR and HRMS. Preliminary in vitro pharmacological tests showed that all target compounds exhibited 5-HT reuptake inhibition activity. Among the tested compounds, 5i, 4a and 5m exhibited potent inhibitory activity against 5-HT reuptake in vitro. It is a chance to find a better precursor of SSRIs (selective serotonin reuptake inhibitors) for further optimization of compounds.

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