Literature DB >> 17127055

Novel carbazole derivatives as NPY Y1 antagonists.

Colin P Leslie1, Romano Di Fabio, Francesca Bonetti, Manuela Borriello, Simone Braggio, Giovanna Dal Forno, Daniele Donati, Alessandro Falchi, Damiano Ghirlanda, Riccardo Giovannini, Francesca Pavone, Angelo Pecunioso, Giorgio Pentassuglia, Domenica A Pizzi, Giovanna Rumboldt, Luigi Stasi.   

Abstract

The synthesis of a series of carbazole derivatives and their SAR at the NPY Y1 receptor is described. Modulation of physicochemical properties by appropriate decoration led to the identification of a high-affinity NPY Y1 antagonist that shows high brain penetration and modest oral bioavailability.

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Year:  2006        PMID: 17127055     DOI: 10.1016/j.bmcl.2006.11.034

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


  1 in total

1.  Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.

Authors:  Shuanghua Hu; Yazhong Huang; Milind Deshpande; Guanglin Luo; Marc A Bruce; Ling Chen; Gail Mattson; Lawrence G Iben; Jie Zhang; John W Russell; Wendy J Clarke; John B Hogan; Astrid Ortiz; Oliver Flint; Andrew Henwood; Qi Gao; Ildiko Antal-Zimanyi; Graham S Poindexter
Journal:  ACS Med Chem Lett       Date:  2012-01-04       Impact factor: 4.345

  1 in total

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