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

Fabio Maria Sabbatini; Romano Di Fabio; Mauro Corsi; Paolo Cavanni; Steve M. Bromidge; Yves St‐Denis; Lucilla D'Adamo; Stefania Contini; Marilisa Rinaldi; Sébastien Guery; Chiara Savoia; Claudia Mundi; Benedetta Perini; Andrew J. Carpenter; Giovanna Dal Forno; Federico Faggioni; Michela Tessari; Francesca Pavone; Carla Di Francesco; Alberto Buson; M. Mattioli; Elisabetta Perdonà; Sergio Melotto

doi:10.1002/cmdc.201000185

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Abstract

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.

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Sabbatini et al. (2010) studied this question.

synapsesocial.com/papers/6a6f6d5bb27f15817826f7df https://doi.org/10.1002/cmdc.201000185

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

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

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