| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1364784 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
Graphical abstractNovel 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. Their synthesis, SAR as well as docking of compound 1 into the 5HT1A receptor model and a model of the 5-HT transporter are discussed.Figure optionsDownload full-size imageDownload as PowerPoint slide
