The Discovery of 4-{1-[({2,5-Dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic Acid (MK-2894), A Potent and Selective Prostaglandin E2 Subtype 4 Receptor A

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• 作者：Marc Blouin ; Yongxin Han ; Jason Burch ; Julie Farand ; Christophe Mellon ; Mireille Gaudreault ; Mark Wrona ; Jean-Franois Lvesque ; Danielle Denis ; Marie-Claude Mathieu ; Rino Stocco ; Erika Vigneault ; Alex
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：March 11, 2010
• 年：2010
• 卷：53
• 期：5
• 页码：2227-2238
• 全文大小：980K
• 年卷期：v.53,no.5(March 11, 2010)
• ISSN：1520-4804

文摘

The discovery of highly potent and selective second generation EP₄ antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. It also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.