Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists

R Di Fabio, R Giovannini, B Bertani, M Borriello…

Index: Di Fabio, Romano; Giovannini, Riccardo; Bertani, Barbara; Borriello, Manuela; Bozzoli, Andrea; Donati, Daniele; Falchi, Alessandro; Ghirlanda, Damiano; Leslie, Colin P.; Pecunioso, Angelo; Rumboldt, Giovanna; Spada, Simone Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 6 p. 1749 - 1752

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Citation Number: 37

Abstract

The SAR of a new series of tetrahydrocarbazole derivatives is described: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat. ... The synthesis and the SAR of new series of NPY-1 antagonists are reported. ... Neuropeptide Y (NPY) is a 36-amino acid peptide isolated from porcine brain in 1982 by Tatemoto et al. 1 NPY belongs to a ...