2. Academic Validation
  3. 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 antagonist

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 antagonist

  • J Med Chem. 2010 Mar 11;53(5):2227-38. doi: 10.1021/jm901771h.
Marc Blouin 1,  Yongxin Han,  Jason Burch,  Julie Farand,  Christophe Mellon,  Mireille Gaudreault,  Mark Wrona,  Jean-François Lévesque,  Danielle Denis,  Marie-Claude Mathieu,  Rino Stocco,  Erika Vigneault,  Alex Therien,  Patsy Clark,  Steve Rowland,  Daigen Xu,  Gary O'Neill,  Yves Ducharme,  Rick Friesen
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada Ltd., 16771 Trans-Canada Highway, Kirkland, QC, Canada. marc_blouin@merck.com
PMID: 20163116 DOI: 10.1021/jm901771h
Abstract

The discovery of highly potent and selective second generation EP(4) 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.

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