Solubilized phenyl-pyrazole ureas as potent, selective 5-HT_2A inverse-agonists and their application as antiplatelet agents

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• 作者：Peter I. Dosa ; Sonja Strah-Pleynet ; Honnappa Jayakumar ; Martin Casper ; Marc Decaire ; Yifeng Xiong ; Juerg Lehmann ; Karoline Choi ; Katie Elwell ; Amy Wong ; Robert R. Webb ; John W. Adams ; Juan Ramirez ; Je
• 关键词：5-HT_2A ; Antiplatelet ; Antithrombosis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 September 2009
• 年：2009
• 卷：19
• 期：18
• 页码：5486-5489
• 全文大小：303 K

文摘

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.