Design, synthesis and antidepressive activity of duloxetine derivatives

In this paper, duloxetine was chosen as the lead compound.  The pharmacophores with 5-HT_1A antagonism activity were used to replace the naphthyl of duloxetine.  A series of duloxetine derivatives had been designed and synthesized and whose structures were confirmed with elemental analysis, MS and ¹H NMR.  All synthesized compounds were tested by tail suspension test and forced swimming test in vivo.  The test   results revealed that most of the compounds have shown better activity than duloxetine at the same dosage.  Some of them are worth to be studied further.