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

The synthesis and the SAR of new series of NPY-1 antagonists are reported. 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...

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Published in	Bioorganic & medicinal chemistry letters Vol. 16; no. 6; pp. 1749 - 1752
Main Authors	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
Format	Journal Article
Language	English
Published	Oxford Elsevier Ltd 15.03.2006 Elsevier
Subjects	Animals Antagonists Biological and medical sciences Biological Availability Carbazoles - chemical synthesis Carbazoles - chemistry Carbazoles - pharmacology CHO Cells - drug effects Cricetinae Cricetulus Drug Evaluation, Preclinical GPCR Humans Male Medical sciences Models, Molecular Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors NPY-1 Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Rats Receptors, Neuropeptide Y - antagonists & inhibitors Receptors, Neuropeptide Y - chemistry Structure-Activity Relationship GPCR Antagonists NPY-1 Intravenous administration Rat Nitrogen heterocycle Non peptide compound Ketoether Structure activity relation Six membered ring Piperidine derivatives Aromatic compound Antagonist Chemical synthesis Carbazole derivatives Rodentia Oral administration Bioavailability Tricyclic compound In vitro In vivo Vertebrata Y1 neuropeptide Y receptor Mammalia Animal Affinity Piperazine derivatives Pharmacokinetics
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Summary:	The synthesis and the SAR of new series of NPY-1 antagonists are reported. 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.11.104