Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation

Fabrizio Micheli; Alessandra Pasquarello; Giovanna Tedesco; Dieter Hamprecht; Giorgio Bonanomi; Anna Checchia; Albert Jaxa-Chamiec; Federica Damiani; Silvia Davalli; Daniele Donati; Chiara Gallotti; Marcella Petrone; Marilisa Rinaldi; Graham Riley; Silvia Terreni; Martyn Wood

doi:10.1016/j.bmcl.2006.05.034

Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3906-12. doi: 10.1016/j.bmcl.2006.05.034. Epub 2006 May 30.

Authors

Fabrizio Micheli¹, Alessandra Pasquarello, Giovanna Tedesco, Dieter Hamprecht, Giorgio Bonanomi, Anna Checchia, Albert Jaxa-Chamiec, Federica Damiani, Silvia Davalli, Daniele Donati, Chiara Gallotti, Marcella Petrone, Marilisa Rinaldi, Graham Riley, Silvia Terreni, Martyn Wood

Affiliation

¹ GlaxoSmithKline Psychiatry Centre of Excellence for Drug Discovery, Via Fleming, 4, 37135 Verona, Italy. fm20244@gsk.com

PMID: 16730983
DOI: 10.1016/j.bmcl.2006.05.034

Abstract

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 molecules are reported.

MeSH terms

Models, Molecular
Pyrroles / chemical synthesis*
Pyrroles / pharmacology*
Pyrrolidinones / chemical synthesis*
Pyrrolidinones / pharmacology*
Serotonin 5-HT2 Receptor Antagonists*
Serotonin Antagonists / chemical synthesis*
Serotonin Antagonists / pharmacology*

Substances

Pyrroles
Pyrrolidinones
Serotonin 5-HT2 Receptor Antagonists
Serotonin Antagonists