Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents

Potent 5-HT(2A) inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5486-5489
Hauptverfasser:	Dosa, Peter I, Strah-Pleynet, Sonja, Jayakumar, Honnappa, Casper, Martin, Decaire, Marc, Xiong, Yifeng, Lehmann, Juerg, Choi, Karoline, Elwell, Katie, Wong, Amy, Webb, Robert R, Adams, John W, Ramirez, Juan, Richman, Jeremy G, Thomsen, William, Semple, Graeme, Teegarden, Bradley R
Format:	Artikel
Sprache:	eng
Schlagworte:	Humans Platelet Aggregation - drug effects Platelet Aggregation Inhibitors - chemistry Platelet Aggregation Inhibitors - pharmacology Pyrazoles - chemistry Pyrazoles - pharmacology Receptor, Serotonin, 5-HT2A - metabolism Serotonin 5-HT2 Receptor Agonists Structure-Activity Relationship Urea - analogs & derivatives Urea - pharmacology
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Beschreibung
Zusammenfassung:	Potent 5-HT(2A) inverse-agonists containing phenyl-pyrazole ureas with an amino side chain were identified. Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2009.07.073