Design, Synthesis and Activity Evaluation of Novel Selective Serotonin Reuptake Inhibitors

Chem. J. Chinese Universities

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Design, Synthesis and Activity Evaluation of Novel Selective Serotonin Reuptake Inhibitors

YANG Jing, WANG Xiao-Fang, DU Guan-Hua, QIN Fang, WEN Hui, YANG Guang-Zhong*

Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

Received:2006-11-02 Revised:1900-01-01 Online:2007-08-10 Published:2007-08-10
Contact: YANG Guang-Zhong

Abstract

Abstract: Depression is a kind of common and severe mental illness. During the past two decades, selective serotonin reuptake inhibitors(SSRIs) have been proved to be a safer and more effective resistance than the first-generation antidepressants(TCAs and MAOIs), and have gained incredible popularity.Based on the conformation analysis and pharmacophore information of SSRIs, flexible database searching from the NCI-3D and Maybridge-3D database was performed. Three classes of the new compounds structures were designed and 27 analogues were prepared and evaluated as potential antidepressant agents. Biphenylbenzamidine derivative Ⅰ-19 showed good activity of affinity to the 5-HT transporter. It can be used as the lead structure for drug design with the objective of making more potent inhibitors against 5-HT transporter.

Key words: Selective serotonin reuptake inhibitors(SSRIs), Antidepressants, Pharmcophore

CLC Number:

O626

TrendMD:

YANG Jing, WANG Xiao-Fang, DU Guan-Hua, QIN Fang, WEN Hui, YANG Guang-Zhong*. Design, Synthesis and Activity Evaluation of Novel Selective Serotonin Reuptake Inhibitors[J]. Chem. J. Chinese Universities, doi: .

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Design, Synthesis and Activity Evaluation of Novel Selective Serotonin Reuptake Inhibitors

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