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Synthesis and 5-HT reuptake inhibition activity of biarylbenzamidine derivatives / 药学学报
Acta Pharmaceutica Sinica ; (12): 619-625, 2008.
Article in Chinese | WPRIM | ID: wpr-277786
ABSTRACT
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 1H 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.
Subject(s)
Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Structure-Activity Relationship / Benzamidines / Serotonin / Selective Serotonin Reuptake Inhibitors / Rats, Wistar / Antidepressive Agents Limits: Animals Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2008 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Pharmacology / Structure-Activity Relationship / Benzamidines / Serotonin / Selective Serotonin Reuptake Inhibitors / Rats, Wistar / Antidepressive Agents Limits: Animals Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2008 Type: Article