79333-48-5Relevant articles and documents
Design, synthesis, and optimization of balanced dual NK1/NK 3 receptor antagonists
Hanessian, Stephen,Jennequin, Thomas,Boyer, Nicolas,Babonneau, Vincent,Soma, Udaykumar,Mannoury La Cour, Clotilde,Millan, Mark J.,De Nanteuil, Guillaume
, p. 550 - 555 (2014/06/09)
In connection with a program directed at potent and balanced dual NK 1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pKi values of 8.6 and 8.1, respectively.
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: Synthesis and biological evaluation
Micheli, Fabrizio,Pasquarello, Alessandra,Tedesco, Giovanna,Hamprecht, Dieter,Bonanomi, Giorgio,Checchia, Anna,Jaxa-Chamiec, Albert,Damiani, Federica,Davalli, Silvia,Donati, Daniele,Gallotti, Chiara,Petrone, Marcella,Rinaldi, Marilisa,Riley, Graham,Terreni, Silvia,Wood, Martyn
, p. 3906 - 3912 (2008/12/21)
Within the continuous quest for the discovery of novel compounds able to treat anxiety and depression, the generation of a pharmacophore model for 5-HT2C receptor antagonists and the discovery of a new class of potent and selective 5-HT2C
ARYL AND BIARYL COMPOUNDS HAVING MCH MODULATORY ACTIVITY
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, (2008/06/13)
In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor. An illustrative inventive compound is shown below: