Literature DB >> 19286377

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.

Steven M Bromidge1, Barbara Bertani, Manuela Borriello, Andrea Bozzoli, Stefania Faedo, Massimo Gianotti, Laurie J Gordon, Matthew Hill, Valeria Zucchelli, Jeannette M Watson, Laura Zonzini.   

Abstract

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones have been identified as highly potent 5-HT(1A/B/D) receptor antagonists with and without additional SerT activity and a high degree of selectivity over hERG potassium channels. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization.

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Year:  2009        PMID: 19286377     DOI: 10.1016/j.bmcl.2009.02.056

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Synthesis, docking studies and biological evaluation of benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives on 5-HT1A serotonin receptors.

Authors:  Hernán Pessoa-Mahana; Gonzalo Recabarren-Gajardo; Jenny Fiedler Temer; Gerald Zapata-Torres; C David Pessoa-Mahana; Claudio Saitz Barría; Ramiro Araya-Maturana
Journal:  Molecules       Date:  2012-02-03       Impact factor: 4.411

  1 in total

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