Synthesis and 5-HT reuptake inhibition activity of biarylbenzamidine derivatives.
- Author:
Fang QIN
1
;
Na-Sha WANG
;
Jing YANG
;
Jian-Jun ZHANG
;
Ya-Fang WANG
;
Guang-Zhong YANG
Author Information
1. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antidepressive Agents;
chemical synthesis;
pharmacology;
Benzamidines;
chemical synthesis;
pharmacology;
Male;
Mice;
Rats;
Rats, Wistar;
Serotonin;
analysis;
Serotonin Uptake Inhibitors;
chemical synthesis;
pharmacology;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2008;43(6):619-625
- CountryChina
- Language:Chinese
-
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.
