[Synthesis and 5-HT reuptake inhibition activity of biarylbenzamidine derivatives].
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.
Qin
Fang
F
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Wang
Na-Sha
NS
Yang
Jing
J
Zhang
Jian-Jun
JJ
Wang
Ya-Fang
YF
Yang
Guang-Zhong
GZ
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001550:Benzamidines / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D051381:Rats; D017208:Rats, Wistar; D012701:Serotonin / Q000032:analysis; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D001550:Benzamidines; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors