Discovery Process and Characterization of Novel Carbohydrazide Derivatives as Potent and Selective GHSR1a Antagonists

Ghrelins: don't feed them after dark! A novel class of highly potent and selective growth hormone secretagogue receptor 1a (GHSR1a) antagonists has been identified. The synthesis and preliminary biological investigation, both in vitro and in vivo is described. This compound series is a useful t...

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Veröffentlicht in:	ChemMedChem 2010-09, Vol.5 (9), p.1450-1455
Hauptverfasser:	Sabbatini, Fabio Maria, Di Fabio, Romano, Corsi, Mauro, Cavanni, Paolo, Bromidge, Steve M., St-Denis, Yves, D'Adamo, Lucilla, Contini, Stefania, Rinaldi, Marilisa, Guery, Sebastien, Savoia, Chiara, Mundi, Claudia, Perini, Benedetta, Carpenter, Andrew J., Dal Forno, Giovanna, Faggioni, Federico, Tessari, Michela, Pavone, Francesca, Di Francesco, Carla, Buson, Alberto, Mattioli, Mario, Perdona', Elisabetta, Melotto, Sergio
Format:	Artikel
Sprache:	eng
Schlagworte:	antagonists Cell Line Drug Evaluation, Preclinical eating disorders Feeding and Eating Disorders - drug therapy ghrelin GHSR1a Humans Hydrazines - chemical synthesis Hydrazines - chemistry Hydrazines - therapeutic use Receptors, Ghrelin - antagonists & inhibitors Receptors, Ghrelin - metabolism Structure-Activity Relationship
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Zusammenfassung:	Ghrelins: don't feed them after dark! A novel class of highly potent and selective growth hormone secretagogue receptor 1a (GHSR1a) antagonists has been identified. The synthesis and preliminary biological investigation, both in vitro and in vivo is described. This compound series is a useful tool for further understanding the role of GHSR1a and may provide new approaches for the treatment of a number of pathological conditions associated with eating disorders.
ISSN:	1860-7179 1860-7187
DOI:	10.1002/cmdc.201000185