Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists

This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT(2C) agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compound 11 was active in in vivo models...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5346-5350
Hauptverfasser:	Andrews, Mark D, Green, Martin P, Allerton, Charlotte M N, Batchelor, David V, Blagg, Julian, Brown, Alan D, Gordon, David W, McMurray, Gordon, Millns, Daniel J, Nichols, Carly L, Watson, Lesa
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CHO Cells Cricetinae Cricetulus Dogs Humans Pyrimidinones - chemistry Pyrimidinones - pharmacology Pyrimidinones - therapeutic use Receptor, Serotonin, 5-HT2B - metabolism Receptor, Serotonin, 5-HT2C - metabolism Serotonin 5-HT2 Receptor Agonists Serotonin Receptor Agonists - chemistry Serotonin Receptor Agonists - pharmacology Serotonin Receptor Agonists - therapeutic use Structure-Activity Relationship Urethra - drug effects Urinary Incontinence - drug therapy
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Zusammenfassung:	This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT(2C) agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compound 11 was active in in vivo models of stress urinary incontinence.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2009.07.133