1207861-06-0Relevant articles and documents
The discovery of 4-{l-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]- 3thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin e2 subtype 4 receptor antagonist
Blouin, Marc,Han, Yongxin,Burch, Jason,Farand, Julie,Mellon, Christophe,Gaudreault, Mireille,Wrona, Mark,Lévesque, Jean-Fran?ois,Denis, Danielle,Mathieu, Marie-Claude,Stocco, Rino,Vigneault, Erika,Therien, Alex,Clark, Patsy,Rowland, Steve,Xu, Daigen,o'Neill, Gary,Ducharme, Yves,Friesen, Rick
supporting information; experimental part, p. 2227 - 2238 (2010/08/21)
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.