Novel 5-HT 1A/1B/1D receptors antagonists with potent 5-HT reuptake inhibitory activity

HT Serafinowska, FE Blaney, PJ Lovell…

Index: Serafinowska, Halina T.; Blaney, Frank E.; Lovell, Peter J.; Merlo, Giancarlo G.; Scott, Claire M.; Smith, Paul W.; Starr, Kathryn R.; Watson, Jeannette M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5581 - 5585

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Citation Number: 18

Abstract

Novel 2-methyl-5-quinolinyl-1-piperazinylalkyl-3, 4-dihydro-2H-1, 4-benzoxazin-3-ones showing high affinities for the 5-HT1A/1B/1D receptors coupled with potent 5-HT reuptake inhibitory activity have been discovered. This is the first report describing docking of the lead compound 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl] ethyl}-2H-1, 4-benzoxazin-3 (4H)- one 1, into a model of the 5-HT transporter and the 5-HT1A receptor model.