931414-12-9Relevant articles and documents
Novel carbazole derivatives as NPY Y1 antagonists
Leslie, Colin P.,Fabio, Romano Di,Bonetti, Francesca,Borriello, Manuela,Braggio, Simone,Forno, Giovanna Dal,Donati, Daniele,Falchi, Alessandro,Ghirlanda, Damiano,Giovannini, Riccardo,Pavone, Francesca,Pecunioso, Angelo,Pentassuglia, Giorgio,Pizzi, Domenica A.,Rumboldt, Giovanna,Stasi, Luigi
, p. 1043 - 1046 (2007)
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.